New Products


New products at Cayman:


Intro Product Cat No Image
24.05.13
AAF-CMK (trifluoroacetate salt)
An inhibitor of TPPII
AAF-CMK is an irreversible inhibitor of TPPII commonly used at 10-100 µM. It does not significantly interfere with the chymotrypsin-like activity of the proteasome. AAF-CMK also inhibits bleomycin hydrolase and puromycin-sensitive aminopeptidase when used at 50 µM.
14461
24.05.13
AG-1295
A selective inhibitor of PDGF receptor kinase
AG-1295 is a quinoxaline-type tyrphostin that acts as a potent and selective inhibitor of PDGF receptor kinase in vitro and in Swiss 3T3 cells (IC50s range from 0.3-1 µM). It inhibits PDGF-stimulated DNA synthesis with an IC50 value of 2.5 µM without affecting activity of the EGF receptor.
14529
24.05.13
AP-18
A reversible channel blocker of TRPA1
AP-18 is a channel blocker which reversibly inhibits TRPA1 (IC50 = 3.1, 4.5 µM for human, mouse TRPA1, respectively). It has minimal effect on TRPV1, TRPV2, TRPV3, TRPV4, or TRPM8. AP-18 has been used to study TRPA1 signaling in mice and rats as well as in vitro.
11912
24.05.13
Apafant
A potent, selective PAF receptor antagonist
Apafant is a water soluble, selective platelet-activating factor (PAF) receptor antagonist that inhibits PAF binding to human PAF receptors with a Ki value of 9.9 nM. Apafant displays anti-inflammatory, antiangiogenic, and anticancer activity.
14532
23.05.13
Ac-DEVD-pNA
A colorimetric caspase substrate
Ac-DEVD-pNA is a para-nitro aniline chromophore cleaved by caspases (Km = 18, 11, 32, 180, and 12 µM for caspases-1, -3, -4, -6, and -7, respectively). It is not cleaved by caspase-2. Cleavage is monitored colorimetrically at 405 nm.
14460
23.05.13
Adenosine 5'-triphosphate (sodium salt)
An essential energy substrate for cellular metabolism
Adenosine 5'-triphosphate (ATP) is a central component of energy storage and metabolism in vivo, providing the metabolic energy to drive metabolic pumps and serving as a coenzyme in a wide array of enzymatic reactions. ATP is a substrate for kinases involved in cell signaling and of adenylate cyclases that produce the second messenger cAMP. It is utilized in various cellular processes including, respiration, biosynthetic reactions, motility, and cell division.
14498
23.05.13
Cordycepin
A nucleoside analog that inhibits polyadenylation
Cordycepin is a nucleoside analog found in C. sinensis that acts as a polyadenylation inhibitor when converted to 3'-deoxyadenosine triphosphate, which inhibits ATP-dependent DNA and RNA synthesis. Cordycepin has a broad spectrum of biological activities, including anti-proliferative, pro-apoptotic, and anti-inflammatory effects. Cordycepin has been shown to reduce poly(A) tail length in mRNA at 10 μM and to activate AMPK kinase, leading to a reduction in mTOR signaling at 200 μM.
14426
23.05.13
Coumarin Boronic Acid
A fluorescent probe for direct detection of ONOO-
Coumarin boronic acid (CBA) is a fluorescent probe that reacts directly and rapidly with ONOO-. ONOO- oxidizes CBA stoichiometrically at a 1:1 ratio into a fluorescent product that can be examined at an excitation of 332 nm and emission >400 nm.
14051
23.05.13
Darifenacin (hydrobromide)
A muscarinic receptor antagonist
Darifenacin is a receptor antagonist acting at the muscarinic receptors (Ki = 5.5, 47, 0.84, 8.6, and 2.3 nM for M1 through M5, respectively). It is effective in treating problems related to the lower urinary tract, including incontinence and overactive bladder.
14424
23.05.13
Doxycycline Hyclate
An antibiotic used in inducible gene expression systems
Doxycycline hyclate is a tetracycline-like antibiotic which effectively controls or prevents a diverse array of infections, including anthrax, Lyme disease, malaria, and Brucellosis. In genetic engineering, doxycycline is used as the regulator for inducible gene expression systems, whereby expression depends on either the presence (Tet-On) or absence (Tet-Off) of doxycycline. Also, doxycycline inhibits certain matrix metalloproteinases (MMP), such as MMP-8 (Ki = 36 µM). It only poorly inhibits MMP-1 and MMP-13 (Ki > 100 µM).
14422
23.05.13
Fluorouracil
A pyrimadine analog that inhibits DNA synthesis
Fluorouracil is a pyrimadine analog that irreversibly inhibits thymidylate synthase, blocking the synthesis of thymidine which is required for DNA synthesis. Intracellular metabolites of fluorouracil exert cytotoxic effects by either inhibiting thymidylate synthetase, or through incorporation into RNA and DNA, ultimately initiating apoptosis. Fluorouracil has been widely used to treat many gastrointestinal tract adenocarcinomas. However, its clinical application is greatly limited due to drug resistance.
14416
23.05.13
Melatonin
An indoleamine neurohormone that entrains circadian rhythms
Melatonin is an indoleamine neurohormone whose levels vary in a daily cycle, thereby allowing the entrainment of the circadian rhythms of several biological functions in animals, plants, and microbes. Many biological effects of melatonin are transduced through melatonin receptors, including the MT1, MT2, and MT3 subtypes. Melatonin also acts as a powerful antioxidant that protects lipids, proteins, and DNA against oxidative damage. Glutathione peroxidase, superoxide dismutases, and catalase are upregulated by melatonin, and melatonin scavenges free radicals as a terminal antioxidant.
14427
22.05.13
ATAD2 bromodomain (human recombinant)
Source: Recombinant N-terminal GST-tagged protein expressed in E. coli · Mr: 43.1 kDa ·
14490
22.05.13
Coumarin Boronic Acid pinacolate ester
A fluorescent probe for detection of hydrogen peroxide
The pinacolate ester of coumarin boronic acid (CBA) reacts with hydrogen peroxide to form the highly fluorescent 7-hydroxycoumarin (umbelliferone), which can be monitored spectrophotometrically (excitation at 335 nm, emission at 450 nm). Through acid hydrolysis CBA pinacolate ester can be used to prepare CBA (Item No. 14051), a fluorescent probe for direct detection of peroxynitrite.
10818
22.05.13
Oil Red O
A lipid staining dye
Oil Red O is used to stain lipids, neutral triglycerides, and some lipoproteins, particularly in cells in culture or in tissues. It is commonly used to evaluate adipogenesis in vitro, as it stains lipid droplets in adipocytes. Oil Red O also positively stains lipid-laden foam cells and lipids in smooth muscle fibers. Staining with Oil Red O can be quantified by measuring absorbance at 490-520 nm.
14419
21.05.13
8-bromo-cAMP (sodium salt)
A PKA activator
8-bromo-cAMP is a cell permeable analog of cAMP that activates cyclic-AMP-dependent protein kinase with a Ka value of 0.05 μM. It activates cyclic-GMP- dependent protein kinase (Ka = 5.8 μM) with 100-fold reduced potency. 8-bromo-cAMP is more stable to hydrolysis and has increased membrane permeability compared to unmodified cAMP.
14431
21.05.13
8-CPT-cAMP (sodium salt)
A cell-permeable cAMP analog
8-CPT-cAMP is a lipophilic activator of the cyclic-AMP- and cyclic-GMP-dependent protein kinases, PKA and PKG (Ka = 0.05 and 0.11 μM, respectively). 8-CPT-cAMP inhibits cyclic GMP-specific phosphodiesterase (PDE VA), cyclic GMP-inhibited phosphodiesterase (PDE III), and cyclic AMP-specific phosphodiesterase (PDE IV) with IC50 values of 0.9, 24, and 25 μM, respectively. It has been used in studies to analyze the signal transduction pathways initiated by cyclic-AMP- and cyclic-GMP-dependent protein kinases.
12011
21.05.13
Buthionine Sulfoximine
An irreversible inhibitor γ-glutamylcysteine synthetase
Buthionine sulfoximine (BSO) is an irreversible inhibitor γ-glutamylcysteine synthetase (Ki <100 μM), the rate-limiting enzyme for L-glutathione (GSH) synthesis, that induces oxidative stress in cells by depleting GSH. Administration of BSO leads to decreased GSH levels in virtually all tissues and is associated with tissue damage and apoptosis. Whereas elevated glutathione levels are associated with tumor cell resistance, BSO has been shown to enhance the toxicity of various chemotherapeutic agents in drug-resistant tumors.
14484
21.05.13
NMDA
An excitatory neurotransmitter
NMDA is a synthetic amino acid derivative that acts as a specific agonist at the NMDA receptor, mimicking the excitatory action of the endogenous ligand glutamate. Signaling through the NMDA receptor influences both neuronal plasticity and neurotoxicity. Repetitive activation of NMDA synapses leads to long-term potentiation, which is used as a model of learning and the initial stages of memory formation.
14581
20.05.13
A-438079 (hydrochloride)
An antagonist of the nucleotide receptor P2X7
A-438079 is a competitive antagonist of the nucleotide receptor P2X7 (pIC50 = 6.9). It inhibits both calcium flux and IL-1β release mediated by P2X7 while not affecting the activity of other P2X receptors. A-438079 is effective in evaluating the role of P2X7 in nociception, oxidative stress, and apoptosis in cells and animals.
14580
20.05.13
Hydroxy Bupropion
A racemic mixture of buproprion metabolites
Hydroxy bupropion is a mixture of enantiomers produced by the metabolism of buproprion by cytochrome P450 2B6. Compared with buproprion, this racemic mixture produces equal inhibition of norepinephrine reuptake (IC50 = 1.7 µM) and much weaker inhibition of dopamine reuptake (IC50 > 10 µM). Moreover, hydroxyl bupropion isomers are potent antagonists of nicotinic receptors, suggesting that they may substitute for bupropion in smoking cessation.
9000522
20.05.13
Pyronin Y
A fluorescent probe for dsRNA
Pyronin Y is a fluorescent probe which stains double stranded RNA in living or fixed cells as well as in tissues. When used in living cell preparations, it is commonly combined with 50-100 µM verapamil to prevent efflux of the dye. It has been used to ascertain the cell cycle state of stem cells and is amenable to flow cytometry. Maximum excitation is at 540-550 nM, with maximum emission at 560-580 nm.
14488
17.05.13
Fluoxetine (hydrochloride)
An SSRI used to treat depression
Fluoxetine is a selective serotonin reuptake inhibitor, displaying a marked preference for the serotonin tranporter (Kd = 0.81 nM) over the norepinephrine transporter (Kd = 240 nM) and the dopamine transporter (Kd = 3600 nM). It is effective in the clinical treatment of major depression as well as other psychiatric disorders.
14418
17.05.13
Idarubicin (hydrochloride)
Antitumor antibiotic used in treatment of leukemia
Idarubicin is a 4-demethoxy analog of the leukemia therapeutic daunorubicin (Item No. 14159). Both are anthracycline antibiotics which intercalate in DNA and inhibit topoisomerase II, resulting in cancer cell cytotoxicity at low concentrations (IC50 = 20-120 nM for idarubicin). Idarubicin is effective in combination therapy for the treatment of different types of leukemia.
14176
17.05.13
Minocycline (hydrochloride)
A broad-spectrum tetracycline antibiotic
Minocycline is a broad-spectrum tetracycline antibiotic which has a particularly long half-life in serum. It is commonly used in the treatment of acne in older patients. Minocycline also has both anti-inflammatory and neuroprotective actions.
14454
17.05.13
Phloretin
A natural inhibitor of various transporters
Phloretin is a natural phenol which inhibits a variety of transporters. It inhibits the monocarboxylate transporters MCT1 and MCT2 (IC50 = 28 and 14 µM, respectively), restricting the rapid transport of monocarboxylates like lactate and pyruvate across the plasma membrane. Phloretin also blocks the sodium/D-glucose cotransporter (Ki = 86 µM) and the human concentrative nucleoside transporter 3 (Ki = 32 µM).
14452
17.05.13
TBB
An inhibitor of CK2
TBB is an ATP/GTP-competitive inhibitor of casein kinase 2 (CK2; IC50 = 900 µM for rat liver CK2). It less potently inhibits CCK2/cyclin A, GSK3β, and phosphorylase kinase (IC50 = 15.6, 11.2, and 8.7 mM, respectively). It is much less effective against a range of other kinases.
14453
17.05.13
Δ4-Dafachronic Acid
A DAF-12 ligand that controls C. elegans development and lifespan
Δ4-Dafachronic acid is a racemic version of a sterol-derived hormone that acts as a ligand of DAF-12. Δ4-Dafachronic acid binds to and transactivates DAF-12, rescuing hormone deficiency in transgenic dauer larvae and promoting reproductive maturation into adults. The (25S) diastereomer of Δ4-dafachronic acid is significantly more potent than its (25R) counterpart (EC50s = 23 and 66 nM, respectively).
14100
15.05.13
LY2183240 2’-isomer
An inhibitor of anandamide uptake
LY2183240 2’-isomer is a less potent, 2,5-regioisomer of LY2183240 that inhibits anandamide hydrolysis and uptake with IC50 values of 33 and 998 nM, respectively.[15431}
14523
15.05.13
ZLN005
A small molecule activator of PGC-1α expression
ZLN005 is a small molecule that stimulates the expression of PGC-1α and downstream genes in skeletal muscle cells, improving glucose utilization and fatty acid oxidation at a concentration of 20 μM. Chronic administration of 15 mg/kg/day ZLN005 to diabetic db/db mice increased PGC-1α and downstream gene transcription in skeletal muscle, increasing fat oxidation and improving glucose tolerance, pyruvate tolerance, and insulin sensitivity.
14121
14.05.13
LY2183240
A potent inhibitor of anandamide uptake
LY2183240 is a potent, competitive small molecule inhibitor of anandamide uptake (IC50 = 270 pM; Ki = 540 pM) and hydrolysis. It has been shown to increase anandamide levels in rat cerebellum (ED50 = 1.37 mg/kg) and displays dose-dependent efficacy (3-30 mg/kg) in several rodent models of persistent pain.
10008663
14.05.13
Ro 25-6981 Maleate
A potent, NR2B-selective NMDA receptor antagonist
Ro 25-6981 maleate is a potent, selective activity-dependent blocker of NMDA receptors containing the NR2B subunit (IC50s = 9 nM and 52 μM for cloned receptor subunit combinations NR1C/NR2B and NR1C/NR2A, respectively). Ro 25-6981 Maleate displays neuroprotectant effects in vitro, protecting cortical neurons against glutamate toxicity and combined oxygen and glucose deprivation with IC50 values of 0.4 and 0.04 μM, respectively.
14578
14.05.13
Z-FA-FMK
An inhibitor of cysteine proteases, including cathepsin B
Z-FA-FMK is an irreversible inhibitor of cysteine proteases, including cathepsins B, L, and S, cruzain, and papain. It also inhibits effector caspases-2, -3, -6, and -7 (IC50 = 6-32 µM) without affecting the initiator caspases-8 and -10. Z-FA-FMK also modulates infection by certain bacteria, parasites, and viruses. It can be used both in cells and in vivo.
14462
14.05.13
Z-VAD(OMe)-FMK
A cell-permeable caspase inhibitor
Z-VAD(OMe)-FMK is a cell-permeable, competitive, and irreversible inhibitor of all caspases. Through this action, it inhibits cleavage of poly (ADP-ribose) polymerase, preventing apoptosis when used at 10-50 µM. It also blocks caspase-mediated apoptosis in vivo. Z-VAD(OMe)-FMK effectively prevents caspase action in inflammasomes.
14463
13.05.13
Ac-DEVD-AFC
A fluorogenic caspase subsrate
Ac-DEVD-AFC is a fluorogenic substrate for activated caspase-3 (Km = 9.7 µM), as well as related caspases. Caspase activity can be quantified by fluorescent detection of free AFC (also known as 7-amino-4-trifluoromethylcoumarin), which is excited at 400 nm and emits at 505 nm.
14459
13.05.13
Ac-DEVD-CMK
An inhibitor of caspase-3
Ac-DEVD-CMK is a cell-permeable, and irreversible inhibitor of caspase-3 as well as caspase-6, -7, -8, and -10. It is commonly used at concentrations up to 100 μM to examine the role of caspase-3-dependent apoptosis in biological systems.
14465
13.05.13
Caspase-3/7 Inhibitor I
An isatin sulfonamide-based inhibitor of caspase-3 and caspase-7
Caspase-3/7 inhibitor I is a potent, reversible, isatin sulfonamide-based inhibitor of caspase-3 (Ki(app) = 60 nM; IC50 = 120 nM) and caspase-7 (Ki(app) = 170 nM). It is a weaker inhibitor of caspase-9 (Ki(app) = 3.1 μM) and caspase-1, caspase-2, caspase-4, caspase-6, and caspase-8 (Ki(app)s ≥25 μM). Caspase-3/7 inhibitor I inhibits apoptosis in camptothecin-treated Jurkat cells (IC50 = ~50 µM) and in chondrocytes (44% inhibition at 10 µM and 98% inhibition at 50 µM). The basis for the unique selectivity of this compound for caspases 3 and 7 involves the recognition of three distinct hydrophobic residues in the S2 pocket surrounding the catalytic cysteine residue.
14464
13.05.13
Diazoxide
A potassium channel activator
Diazoxide is a potassium channel activator that causes local relaxation in smooth muscle by increasing membrane permeability to potassium ions. The cellular release of potassium switches off voltage-gated calcium ion channels which inhibits the generation of an action potential. Diazoxide relaxes rat aorta rings with an ED50 value of 19.3 μM and has been used as a vasodilator in the treatment of hypertension. Diazoxide also decreases the secretion of insulin by activating pancreatic β cell potassium channels and, thus, it has been used to counter hypoglycemia in certain disease states.
14576
13.05.13
Interleukin-17A (mouse) EIA Kit
Enzyme immunometric assay for the measurement of mouse IL-17A
Interleukin-17A (IL-17A or CTLA-8) is produced by TH17 cells, a helper CD4 T cell lineage distinct from TH1 (producing IFNγ) and TH2 (producing IL-4, IL-5, and IL-13). IL-17A acts in a variety of cell types to induce the production of acute-phase proteins, antimicrobial proteins, and neutrophil-activating factors. It is especially important for antimicrobial responses and plays a role in the pathogenesis of several mouse models of human chronic inflammatory disease including collagen induced arthritis, experimental autoimmune encephalomyelitis, and asthma. Cayman’s IL-17A (mouse) EIA Kit is an immunometric (i.e., sandwich) EIA that permits IL-17A measurements within the range of 0-1,000 pg/ml, with a lower limit of quantification (LLOQ) of 15.6 pg/ml.
500970
13.05.13
Purvalanol A
A selective inhibitor of cyclin-dependent kinases
Purvalanol A is a potent, cell-permeable, and selective inhibitor of cyclin-dependent kinases with IC50 values of 4, 70, 35, 850, and 75 nM for cdc2/cyclin B, cdk2/cyclin A, cdk2/cyclin E, cdk4/cyclin D1 and cdk5-p35, respectively. Purvalanol A reversibly arrests synchronized cells in the G1 and G2 phase of the cell cycle, inhibiting both cell proliferation and cell death. At 10 μM, purvalanol A potently suppresses the anchorage-independent growth of c-Src-transformed cells as well as HT29 and SW48 human colon cancer cells.
14579
13.05.13
Riluzole (hydrochloride)
An inhibitor of glutamatergic transmission
Riluzole is a benzothiazole derivative with anti-excitotoxic effects that acts by blocking the presynaptic release of glutamate, indirectly antagonizing glutamate receptors, and inactivating neuronal voltage-gated Na+ channels (ED50 = 2.3 μM). Riluzole suppresses glutamate-induced seizures in rats at an ED50 value of 3.2 mg/kg and displays neuroprotective effects in hypoxic animals at an ED50 value of 4 mg/kg. Riluzole has been explored as a therapeutic for slowing disease progression of amyotrophic lateral sclerosis.
14577
13.05.13
SIRT1/2 Inhibitor IV
Cell-permeable inhibitor of SIRT1 and SIRT2
SIRT1/2 Inhibitor IV is a cell-permeable inhibitor of SIRT1 (IC50 = 56 µM) and SIRT2 (IC50 = 59 µM), blocking NAD+-dependent deacetylase activity in a substrate competitive manner. It less effectively inhibits SIRT5 (IC50 >300 µM) and has no effect on class I and II histone deacetylases. By inhibiting SIRT1, SIRT1/2 Iinhibitor IV sensitizes H460 lung cancer cells to etoposide and paclitaxel and enhances etoposide-induced G2 arrest. It also blocks a SIRT1-dependent hypoxic response in vivo, suppressing HIF-1α protein accumulation as well as EPO and VEGF expression in HepG2 tumors in mice.
14407
09.05.13
CAY10669
An inhibitor of pCAF
CAY10669 is an inhibitor of the histone acetyltransferase pCAF (p300/CREB-binding protein-associated factor; IC50 = 662 μM), displaying a 2-fold improvement in inhibitory potency over anacardic acid (Item No. 13144). At 30-60 μM, CAY10669 can dose-dependently inhibit histone H4 acetylation in HepG2 cells in vitro.
10974
09.05.13
Chloramphenicol
A broad-spectrum antibiotic
Chloramphenicol is a broad-spectrum antibiotic that is effective against both Gram-positive and Gram-negative bacteria including H. influenzae, N. meningitides, N. gonorrhoeae, S. typhi, Brucella species, and B. pertussis strains. Chloramphenicol disrupts bacterial protein synthesis by preventing chain elongation through the inhibition of the peptidyl transferase activity of the bacterial 50S ribosome.
14334
09.05.13
Ciprofloxacin (hydrochloride)
A fluoroquinolone antibiotic with antimicrobial and immunomodulatory effects
Ciprofloxacin is a fluoroquinolone antibiotic that is widely used as an antimicrobial and immunomodulatory agent. Its range of activity includes most strains of bacterial pathogens capable of inducing respiratory, urinary tract, gastrointestinal, and abdominal infections. It functions by inhibiting DNA gyrase (a type II topoisomerase) and topoisomerase IV, the enzymes responsible for negative supercoiling of chromosomes and DNA strand separation, thus blocking initiation of bacterial replication. Most recently ciprofloxacin has been used in the management of postexposure inhalational anthrax and radiation combined injury resulting from nuclear disasters.{22832;22834}
14286
09.05.13
Magnolol
A CB2 receptor agonist
Magnolol is a bioactive compound isolated from the bark of M. officinalis that has been used in Asian traditional medicine for the treatment of anxiety, sleeping disorders, and allergic diseases. Magnolol can activate cannabinoid (CB) receptors, behaving as a partial agonist with selectivity for the peripheral CB2 subtype (EC50 = 3.28 μM; Ki = 1.44 μM) versus central CB1 (EC50 = 18.3 μM; Ki = 3.15 μM).
14233
09.05.13
MK 25 (hydrochloride)
A highly selective MAPKAPK2 (MK2) inhibitor
MK 25 is a highly selective, non-ATP competitive MK2 inhibitor with an IC50 value of 0.11 μM. MK 25 has been shown to inhibit pro-inflammatory cytokine secretion from the human THP1 acute monocytic leukemia cell line, causing inhibition of LPS-stimulated TNF-α (IC50 = 4.4 μM) and IL-6 (IC50 = 5.2 μM) secretion. It can also inhibit IL-1β-stimulated matrixmetalloprotease 13 secretion from the SW1353 chondrosarcoma cell line (IC50 = 5.7 μM) and human primary chondrocyte cultures (IC50 = 2.2 μM).
14399
09.05.13
Ponceau S (sodium salt)
A protein stain
Ponceau S is a stain that permits the rapid, reversible detection of proteins immobilized on various matrices, including nitrocellulose and polyvinylidene fluoride membranes. It can be used to locate proteins or evaluate efficiency of transfer. Reversible staining with ponceau S has also been validated as an alternative to actin probing as a loading control. This stain can also be used as a fiducial marker in mass spectrometric imaging.
14330
09.05.13
Tetrahydromagnolol
A CB2 receptor agonist
Tetrahydromagnolol is a major metabolite of magnolol that is 19-fold more potent than magnolol as a peripheral CB2 receptor agonist (EC50 = 0.17 μM; Ki = 0.42 μM). It also behaves as an antagonist at GPR55, a CB-related orphan receptor (KB = 13.3 μM).
14234
08.05.13
Amiloride (hydrochloride)
A potassium-sparing diuretic
Amiloride is a potassium-sparing diuretic that promotes the loss of sodium and water from the body by directly blocking sodium reabsorption through epithelial sodium channels. Amiloride can also block Na+/H+ exchangers in the heart, which can serve to minimize reperfusion injury in ischemic attacks. Additionally, acid-sensing ion channels, which are involved in nociceptor responses to pH, can also be inhibited by amiloride.
14409
08.05.13
Dantrolene (sodium salt)
A skeletal muscle relaxant that binds type 1 ryanodine receptors
Dantrolene is a skeletal muscle relaxant that depresses excitation-contraction coupling in skeletal muscle by binding to the type 1 ryanodine receptor and decreasing free intracellular calcium concentration. Dantrolene (10 μM) inhibits L-type currents in developing myotubes by shifting the voltage-dependence of skeletal L-type Ca2+ channel activation to more depolarizing potentials. It has been used for the treatment of malignant hyperthermia, the management of neuroleptic malignant syndrome, spasticity, and Ecstasy intoxication.
14326
08.05.13
Efavirenz
A potent non-nucleoside reverse transcriptase inhibitor
Efavirenz is an NNRTI that prevents RNA plus-strand initiation with an IC50 value of 17 nM. Efavirenz also inhibits the late stages of HIV-1 replication by interfering with HIV-1 Gag-Pol polyprotein processing. It has been used in combination therapy with drugs directed at the treatment of opportunistic infections such as HIV and cancer.
14412
08.05.13
L-AP4
A selective Group III metabotropic glutamate receptor agonist
L-AP4, an analog of L-glutamic acid, is a selective Group III mGluR agonist that functions presynaptically to suppress glutamate release (IC50 = 2.5 μM). L-AP4 has been shown to depress synaptic transmission in glutamatergic pathways in the hippocampus, olfactory bulb, and retina as well as act as an agonist at the quisqualate-sensitized AP6 site in hippocampus.
14538
08.05.13
MPEP (hydrochloride)
A potent, highly selective mGlu5a receptor antagonist
MPEP is a potent, highly selective non-competitive antagonist at the mGlu5a receptor subtype (IC50 = 36 nM) while having no agonist or antagonist activities at the mGlu1b receptor at concentrations up to 30 μM. MPEP is centrally active following systemic administration in vivo, inducing anxiolytic-like effects in rodent models of anxiety and depression when administered at 1-30 mg/kg. MPEP has also been reported as a positive allosteric modulator of mGluR4 at μM concentrations.
14536
08.05.13
PPADS (sodium salt)
A non-selective P2-purinoceptor antagonist
PPADS is a non-selective P2 purinergic antagonist that blocks recombinant P2X1-5 (IC50s = 1-2.6 μM), native P2Y2-like (IC50 = ~0.9 mM), and recombinant P2Y4 (IC50 = ~15 mM) receptors. PPADS antagonism of ATP-sensitive P2 receptors produces neuroprotective effects in an ischemia model with permanent middle cerebral artery occlusion in spontaneously hypertensive rats.
14537
08.05.13
Resazurin (sodium salt)
A dye used as an oxidation-reduction indicator
Resazurin is a blue non-fluorescent dye that when reduced to the highly red-fluorescent product resorufin (excitation: 530-540 nm; emission: 585-595 nm) can be used as a quantifiable detection agent for enzyme activity assays. The non-fluorescent resazurin can be used as an oxidation-reduction indicator in cell viability assays in a variety of cells.
14322
08.05.13
Tetracycline (hydrochloride)
A selective antibiotic used in cell culture systems
Tetracycline is a broad-spectrum antibiotic that prevents bacterial growth by inhibiting protein synthesis. It binds to a single site in the 30S ribosomal subunit which prevents attachment of aminoacyl tRNA to the ribosomal acceptor site. It is used in cell biology as a selective agent in cell culture systems. Tetracycline is toxic to prokaryotic and eukaryotic cells and selects for cells harboring the bacterial tetR gene, which are resistant to the antibiotic.
14328
07.05.13
BRD2 bromodomains 1 and 2 TR-FRET Assay Kit
High Throughput Screening assay for BRD2 inhibitors
Bromodomains recognize acetylated lysine residues and recruit regulatory complexes to acetylated nucleosomes, thereby controlling chromatin structure and gene expression. The isolated individual or tandem bromodomains of BRD2 and BRD4 bind acetylated histone tails, which couple histone acetylation marks to the transcriptional regulation of target promoters. Small molecule inhibitors of bromodomain/histone interactions hold promise as useful therapeutics for human disease. Cayman’s BRD2 bromodomains 1 and 2 TR-FRET Assay Kit is a homogeneous, TR-FRET assay method amenable to rapid characterization of inhibitors of bromodomain/acetylated peptide interaction in a high throughput format. This screening assay is robust, displaying a Z' >0.6.
600810
07.05.13
Bromophenol Blue
A vital dye with multiple utility
Bromophenol blue is commonly used as a pH indicator, a color marker to monitor the progress of agarose or polyacrylamide gel electrophoresis, and a dye to detect proteins and nucleic acids (absorbance at 610 nm), particularly when staining living tissues. As an acid-base indicator its useful pH range is 3-4.6 where the color changes from yellow at pH 3.0 to purple at pH 4.6.
14331
07.05.13
CBP bromodomain TR-FRET Assay Kit
High Throughput Screening assay for CBP inhibitors
CBP (CREB-binding protein or CREBBP) functions as a histone acetyltransferase, catalyzing the transfer of an acetyl group from the cofactor acetylCoA to the ε-amine of a substrate lysine side chain. These acetylated lysine residues are recognized by bromodomains and play a critical role in the epigenetic regulation of gene transcription. CBP has also been shown to acetylate numerous non-histone proteins including various transcription factors and coactivators, some of which are related to several oncogenes and tumor suppressors. Cayman’s CBP bromodomain TR-FRET Assay Kit is a homogeneous, TR-FRET assay method amenable to rapid characterization of inhibitors of bromodomain/acetylated peptide interaction in a high throughput format. This screening assay is robust, displaying a Z' >0.6.
600850
07.05.13
D-AP5
A selective NMDA antagonist
D-AP5 is a selective N-methyl-D-aspartate (NMDA) receptor antagonist (Kd = 1.4 μM) that competitively inhibits the glutamate binding site of NMDA receptors. Whereas D-AP5 is the active (−)-stereoisomer, its (+)-isomer (L-AP5) demonstrates considerably less potent NMDA receptor antagonist activity. AP5 has been widely used to study the activity of NMDA receptors particularly in regard to researching synaptic plasticity, learning, and memory.
14539
07.05.13
DL-AP5
A competitive NMDA antagonist
DL-AP5 is the racemic version of the selective N-methyl-D-aspartate (NMDA) receptor antagonist, D-AP5 (Item No. 14539). Whereas D-AP5 is the active (−)-stereoisomer that competitively inhibits the glutamate binding site of NMDA receptors (Kd = 1.4 μM), the (+)-isomer (L-AP5) demonstrates considerably less potent NMDA receptor antagonist activity. AP5 has been widely used to study the activity of NMDA receptors particularly in regard to researching synaptic plasticity, learning, and memory.
14540
07.05.13
Phenylmethylsulfonyl fluoride
A nonspecific, irreversible serine protease inhibitor
Phenylmethylsulfonyl fluoride (PMSF) is a nonspecific, irreversible inhibitor of serine proteases and other enzymes, including acetylcholinesterase, palmityl coenzyme A deacylase, arylsulfatase A, chymotrypsin, and trypsin. It is used in protein solublization studies in order to deactivate proteases from digesting proteins of interest after cell lysis. Because PMSF specifically sulfonylates the hydroxal groups of active site serine residues of enzymes, it can be used as a chemical label to identify essential active site serines in an enzyme. PMSF is known to alter the actions of anandamide by blocking its metabolism and can produce cannabinoid effects in mice, including antinociception, hypothermia, and immobility with ED50 values of 86, 224, and 206 mg/kg, respectively.
14333
07.05.13
Serotonin (hydrochloride)
A tryptophan-based amino acid neurotransmitter
Serotonin is a monoamine neurotransmitter that is biochemically derived from tryptophan and produced in serotonergic neurons in the central nervous system and in enterochromaffin cells in the gastrointestinal tract. Serotonin is important in the regulation of mood, sleep, vomiting, sexuality, and appetite. Low levels of serotonin are associated with several disorders, including depression, migraines, bipolar disorder, and anxiety. Its actions are terminated primarily via uptake of serotonin from the synapse. Serotonin reuptake can be inhibited with MDMA, cocaine, tricyclic antidepressants, and selective serotonin reuptake inhibitors.
14332
06.05.13
Acridine Orange
A fluorescent cationic dye useful for cell cycle determination
Acridine orange is a cell permeable, nucleic acid-selective fluorescent cationic dye useful for cell cycle determination. It emits green fluorescence (excitation maximum: 502 nm; emission maximum: 525 nm) when bound to dsDNA and red fluorescence (excitation maximum: 460 nm; emission maximum: 650 nm) when bound to ssDNA or RNA. Acridine orange will also enter acidic compartments such as lysosomes and become protonated and sequestered. In low pH conditions such as this, acridine orange will emit orange fluorescence (emission ~590 nm) when excited by blue light (475 nm).
14338
06.05.13
Ampicillin (sodium salt)
An antibacterial antibiotic
Ampicillin is an antibacterial antibiotic from the α-aminobenzyl penicillin group, which differs from penicillin by the presence of an amino group that facilitates penetration through the outer membrane of some gram-negative bacteria. Ampicillin acts by interfering directly with the biosynthesis of peptidoglycan, which constitutes the major component of the bacterial cell wall, leading to structural instability and death of bacteria. It can be used as a selective antibiotic for resistant bacteria.
14417
06.05.13
J 147
A neuroprotective hybrid of curcumin
J 147, a hybrid of curcumin (Item No. 81025) and the neurotrophic compound, cyclohexyl-bisphenol A, displays broad neuroprotective activity (EC50 = 25 nM) in a panel of assays representing neurotoxicity pathways related to aging and neurodegenerative disease. J 147 has been shown to enhance memory in normal animals and to prevent memory deficits in an Alzheimer’s disease mouse model. These effects are associated with an increase in brain derived neurotrophic factor levels, enhanced long-term potentiation, preservation of synaptic proteins, a reduction of markers for oxidative stress and inflammation, a reduction of amyloid plaques, and lower levels of soluble amyloid β.
14451
06.05.13
Palmitelaidic Acid
The trans isomer of palmitoleic acid
Palmitelaidic acid is the trans isomer of the 16:1 fatty acid palmitoleic acid. While its effects on cholesterol levels are poorly studied, palmitelaidic acid can have very different effects from those of palmitoleic acid on lipid metabolism and mobilization.
9001798
06.05.13
Palmitelaidic Acid methyl ester
The trans isomer of palmitoleic acid
Palmitelaidic acid methyl ester is an ester version of the free acid which may be more amenable for the formulation of fatty acid-containing diets and dietary supplements.
9001797
06.05.13
TAF1 bromodomain 2 (human recombinant)
Source: recombinant N-terminal GST-tagged protein expressed in E. coli · Mr: 43.5 kDa ·
14495
03.05.13
AEBSF (hydrochloride)
An irreversible serine protease inhibitor
AEBSF is a water soluble, irreversible, broad spectrum inhibitor of serine proteases, including trypsin, chymotrypsin, plasmin, thrombin, and kallikreins. AEBSF can also prevent the activation of the ROS generator, NADPH oxidase. At 10-50 μg, AEBSF can attenuate airway inflammation in a mouse model of airway allergy. AEBSF maintains stability in slightly acidic aqueous solutions and serves as a nontoxic alternative to the organophosphate inhibitors, PMSF and DFP.
14321
03.05.13
Brilliant Blue G
A dye for staining or quantifying proteins
Brilliant Blue G is a dye which is commonly used in laboratories to stain or quantify proteins. A variety of methods have been developed for using Brilliant Blue G to stain gels with ease and sensitivity. The Bradford assay is a standard, rapid dye-binding assay that uses Brilliant Blue G to quantify the amount of protein in a solution. This compound also acts as a selective inhibitor of the P2X purinoceptor channel P2X7 (IC50s = 10.1 and 265 nM for rat and human P2X7, respectively). In mice, it inhibits interleukin-1β expression and reduces neurological injury secondary to traumatic brain injury.
14320
03.05.13
Dapagliflozin
A sodium-glucose cotransporter (SGLT) inhibitor
Dapagliflozin is a first generation, selective sodium-glucose cotransporter (SGLT) inhibitor that blocks glucose transport with about 100-fold selectivity for SGLT2 (Ki = 6 nM; EC50 = 1.1 nM) over SGLT1 (Ki = 390 nM). After single oral doses ranging from 0.1 to 1.0 mg/kg, dapagliflozin increases urinary glucose excretion in both normal and diabetic rats, improves glucose tolerance in normal rats, and reduces hyperglycemia in Zucker diabetic fatty rats. Within two weeks of treating diabetic rats with 0.1 to 1.0 mg/kg dapagliflozin, fasting and fed glucose levels have been shown to be significantly lowered as a result of increased glucose utilization accompanied by reduced glucose production.
11574
03.05.13
DAPI (hydrochloride)
A fluorescent DNA probe
DAPI is a fluorescent probe which is commonly used to stain DNA and chromosomes for fluorescent microscopy and flow cytometry applications. It forms a fluorescent complex by attaching in the minor groove of A-T rich sequences of DNA. DAPI is often used as a counterstain, as its ultraviolet (max 358 nm) excitation and blue (max 461 nm) emission wavelengths separate it nicely from many popular primary fluorophores. It can be used on either fixed or live cells, although its low permeability in live cells demands that higher concentrations be used.
14285
03.05.13
Diphenhydramine (hydrochloride)
An antagonist of histamine and muscarinic receptors
Diphenhydramine (DPH) is a first generation antihistamine which is a potent antagonist of the human H1 receptor (Ki = 11.7 nM). Like many first generation antihistamines, DPH readily crosses the blood-brain barrier and produces diverse cognitive and psychomotor effects. DPH also antagonizes muscarinic cholinergic receptors (Ki = 100 to 260 nM for M1 through M5), increasing the range of central nervous system effects and applications.
11158
03.05.13
Fast Green FCF
A dye used to stain proteins for IEF and SDS-PAGE
Fast Green FCF is a dye used to stain proteins for IEF (isoelectric focusing) and SDS-PAGE. When bound to proteins, Fast Green FCF fluoresces near infrared (absorption maximum: 624 nm). Fast Green FCF staining is linear over a wider range of protein concentrations compared to Brilliant Blue R.
14335
03.05.13
Gatifloxacin
A fluoroquinolone antibiotic
Gatifloxacin is a fluoroquinolone antibiotic which inhibits bacterial DNA gyrase (IC50 = 0.109 μg/ml) and topoisomerase IV (IC50 = 13.8 μg/ml). It is much less effective against HeLa cell topoisomerase II (IC50 = 265 μg/ml). Gatifloxin has been used as a broad-spectrum oral antibiotic, but it can produce dysglycemia in older adults. It remains useful for resolving bacterial conjunctivitis.
14290
02.05.13
Kartogenin
A potent inducer of chondrocyte differentiation
Kartogenin potently induces differentiation of human mesenchymal stem cells into chondrocytes with an EC50 value of 100 nM. Kartogenin induces chondrogenesis by binding the actin-binding protein, filamin A, which disrupts its interaction with the transcription factor core-binding factor β subunit (CBFβ). When dissociated from filamin A, CBFβ translocates to the nucleus and forms a transcriptional complex with the runt-related transcription factor RUNX1, which enables chondrocyte differentiation. Kartogenin has been shown to promote cartilage repair in a mouse model of osteoarthritis and to protect against cytokine-induced damage in osteoarthritic bovine articular chondrocytes in vitro.
11826
02.05.13
Tolterodine tartrate
An antagonist of muscarinic receptors
Tolterodine tartrate is a competitive antagonist of muscarinic (M) receptors (Ki = 1.4, 2.7, 3.6, 3.1, and 2.2 nM for M1 through M5, respectively). Antagonists of muscarinic receptors, including tolterodine, are effective in treating overactive bladder symptoms.
15027
02.05.13
Varenicline tartrate
A partial agonist of the α4β2 nicotinic receptor
Varenicline tartrate is a partial agonist of the α4β2 neuronal nicotinic acetylcholine receptor (EC50 = 2.3 µM). It shows high selectivity for this receptor subclass relative to other nicotinic receptors, non-nicotinic receptors, and transporters. Varenicline competes with the binding of nicotine. It is effectively used in smoking cessation.
15030
01.05.13
Azithromycin
A macrolide antibiotic
Azithromycin is a macrolide antibiotic with high stability at acidic pH, long half-life, and favorable effectiveness against a range of organisms. In addition, it interferes poorly with the cytochrome P450 system in vitro, limiting side effects related to drug interactions. Azithromycin is effective, in combination with chloroquine, for protection against malaria.
15004
01.05.13
Glycitein
A major isoflavone
Glycitein is an O-methylated isoflavone that comprises 5-10% of the total isoflavones in soy food products. This phytoestrogen is reported to have weak estrogenic activity, displacing estradiol binding at the estrogen receptor in vitro with an IC50 value of 3.94 μM. It suppresses the proliferation of osteoblasts and promotes differentiation from its progenitor. It has also been used to attenuate proliferation (10 μM) of aortic smooth muscle cells related to atherosclerotic vascular change in stroke-prone hypertensive rats and to protect against beta amyloid (Aβ)-induced toxicity and oxidative stress (100 μg/ml) in C. elegans expressing human Aβ.
14162
01.05.13
Temsirolimus
A specific inhibitor of mTOR activity
Temsirolimus is a dihydroxymethyl propionic acid ester of rapamycin with improved solubility that specifically inhibits mTOR signaling with a potency similar to that of rapamycin. Treatment with temsirolimus leads to cell cycle arrest in the G1 phase and also inhibition of tumor angiogenesis by reducing synthesis of VEGF. Temsirolimus demonstrates cytostatic activity in several xenograft models of human tumors in nude mice, including glioblastomas, prostate carcinoma, pancreatic, liver, and breast cancers, and medulloblastoma.
11590
01.05.13
Z-DEVD-FMK
Inhibitor of caspase-3
Z-DEVD-FMK is a cell-permeable irreversible inhibitor of caspase-3 (IC50 = 130 nM). It potently inhibits apoptosis.
14414
29.04.13
5-(N-ethyl-N-isopropyl)-Amiloride
A selective inhibitor of Na+/H+ exchangers
5-(N-ethyl-N-isopropyl)-Amiloride (EIPA) is a potent inhibitor of several NHE isoforms, inhibiting NHE1, NHE2, NHE3, and NHE5 with Ki values of 0.02, 0.5, 2.4, and 0.42 μM, respectively. It less effectively inhibits NHE4 (IC50 ≥10 μM). EIPA is commonly used at a concentration of 5-10 μM to inhibit cellular HNE activity.
14406
29.04.13
A-771726
A selective inhibitor of de novo pyrimidine synthesis
A-771726 is the active metabolite of leflunomide, a prodrug approved by the FDA for treatment of rheumatoid arthritis. A-771726 reversibly inhibits dihydroorotate dehydrogenase, the rate-limiting step in the de novo synthesis of pyrimidines. It prevents activated lymphocytes from accumulating sufficient pyrimidines to support DNA synthesis (IC50s = 0.09, 3.5, and 12.5 μM for rat, mouse, and human, respectively). At higher doses, A-771726 inhibits tyrosine kinases responsible for early T cell and B cell signaling in the G0/G1 phase of the cell cycle. A-771726 has also been shown to inhibit the production of prostaglandin E2 in synoviocytes activated by TNF-α and IL-1α (IC50s = 7 and 3 μM, respectively) as well as inhibit MMP-1 and IL-6 production at concentrations >10 μM.
14404
29.04.13
Entacapone
A peripherally acting, selective and reversible COMT inhibitor
Entacapone is a peripherally acting, selective and reversible COMT inhibitor with IC50 values of 150-300 nM in rat liver (Ki = 145 nM) and 10-20 nM in rat brain tissues. It was designed as an adjuvant to L-DOPA/dopa decarboxylase inhibitor treatment for Parkinson’s disease. Peripheral COMT inhibition with entacapone can decrease 3-OMD levels in the rat brain by 16-52% and prolong the bioavailability of L-DOPA in patients with Parkinson’s disease.
14153
29.04.13
MDL 28170
A cell permeable, selective calpain inhibitor
MDL 28170 is a cell permeable, selective inhibitor of μ-calpain (calpain-1) and m-calpain (calpain-2). MDL 28170 crosses the blood-brain barrier to inhibit brain cysteine protease activity and has been reported to have neuroprotective effects in numerous rodent neurotrauma models, including spinal cord injury, cortical impact trauma, neonatal hypoxia-ischemia, and focal cerebral ischemia. Additionally, MDL 28170 has been shown to attenuate depression in myocardial contractile performance that occurs during reperfusion following cardiac ischemia.
14283
29.04.13
β-Lapachone
An anti-cancer quinone
β-Lapachone is a natural quinone with diverse anti-cancer and anti-inflammatory effects. It inhibits topoisomerase I at 25 μM and transglutaminase (IC50 = 5 μM). In cancer cells which overexpress NAD(P)H:quinone oxidoreductase, β-lapachone is reduced to β-lapachone hydroquinone, which generates reactive oxygen species during its reversion to β-lapachone. This process sensitizes cancer cells to radiation, suppresses NF-κB activation, and drives apoptosis.
15021
26.04.13
7α,25-dihydroxy Cholesterol
A potent and selective agonist of GPR183
7α,25-dihydroxy Cholesterol (7α,25-DHC) is a potent agonist of GPR183 that induces specific activation of the receptor with an EC50 value of 50 nM (Kd = 450 pM). At concentrations below 3 μM, it does not show any appreciable binding activity when tested against eight different nuclear hormone receptors including LXR and thirty-one different G protein-coupled receptors in a panel of reporter gene assays. 7α,25-DHC can act as a potent chemokine, affecting migration of immune cells expressing GPR183 both in vitro (EC50 = 500 pM) and in vivo.
11032
26.04.13
Resolvin D2-d5
An internal standard for the quantification of RvD2
RvD2-d5 contains five deuterium atoms at the 21, 21’, 22, 22, and 22 positions. It is intended for use as an internal standard for the quantification of RvD2 by GC- or LC-mass spectrometry (MS).
11184
25.04.13
GANT 58
An inhibitor of GLI transcription
GANT 58 is a GLI antagonist that inhibits GLI1-mediated transcription (EC50 = 5 μM) in a variety of cell types. It inhibits the hh signaling pathway downstream of Smo and the endogenous downstream inhibitor Sufu thereby affecting GLI1 nuclear accumulation. GANT 58 displays antiproliferative and antitumor activity against Ewing sarcoma family of tumor cells.
14193
25.04.13
Hygromycin B
An antibiotic used to select transformed cells
Hygromycin B is an antibiotic which is used in molecular and cell biology to select for transformed cells expressing the hygromycin resistance gene. It is an aminoglycoside produced by the bacterium S. hygroscopicus which kills prokaryotic and eukaryotic cells by inhibiting protein synthesis. The hygromycin resistance gene (hyg or hph) encodes a phosphotransferase which inhibits hygromycin through phosphorylation.
14291
24.04.13
Cyclophosphamide (hydrate)
An alkylating agent used to treat cancer
Cyclophosphamide is a nitrogen mustard alkylating agent used in the treatment of cancers and autoimmune disorders. In cells with low levels of aldehyde dehydrogenase, cyclophosphamide acts as a prodrug since it is metabolized to the active compound phosphoramide mustard, which crosslinks with DNA and causes cell death.
13849
24.04.13
Neomycin (sulfate)
An antibiotic used in tissue culture studies
Neomycin is an aminoglycoside antibiotic produced by S. fradiae that inhibits protein translation by binding to the small subunit of prokaryotic ribosomes. It blocks voltage-sensitive Ca2+ channels and is a potent inhibitor of skeletal muscle sarcoplasmic reticulum Ca2+ release. Neomycin has been shown to inhibit inositol phospholipid turnover, phospholipase C, and phosphatidylcholine-phospholipase D activity (IC50 = 65 µM). It is highly effective against Gram-positive and Gram-negative bacteria and is commonly used for the prevention of bacterial contamination of cell cultures.
14287
24.04.13
Propidium Iodide
A fluorescent probe used to identify dead cells
Propidium iodide (PI) is membrane impermeant and generally excluded from viable cells. However, it can easily penetrate dead or damaged cells and as such is commonly used for identifying cell viability in a population or as a counterstain in multicolor fluorescent techniques. It binds to DNA and RNA by intercalating between the bases. PI is excited at 488-535 nm with an emission maximum of 617 nm. This probe is suitable for fluorescence microscopy and flow cytometry.
14289
24.04.13
Spectinomycin (hydrochloride hydrate)
An aminocyclitol antibiotic
Spectinomycin is an aminocyclitol antibiotic produced by S. spectabilis that is active against Gram-negative and Gram-positive bacteria. Spectinomycin inhibits protein synthesis by binding to the 30S ribosomal subunit and interfering with peptidyl tRNA translocation. Mutations in the gene for ribosomal protein S5 prevents binding of spectinomycin and contributes to bacterial resistance.
14324
24.04.13
W-13 (hydrochloride)
A potent calmodulin antagonist
W-13 is a naphthalenesulfonamide derivative that acts as a potent antagonist of calmodulin (IC50 = 22 μM) and is widely used to investigate Ca2+/calmodulin-regulated enzyme activities.
14277
23.04.13
2-deoxy-D-Glucose
A widely used inhibitor of glycolysis
2-deoxy-D-Glucose is a non-metabolizable glucose analog that inhibits phosphorylation of glucose by hexokinase, the first step of glycolysis. This results in the depletion in cellular ATP, the inhibition of protein glycosylation, and the disruption of ER quality control by inducing the unfolded protein response. 2-deoxy-D-glucose has been shown to cause cell cycle inhibition and cell death in in vitro models of hypoxia, induce autophagy, increase reactive oxygen species production, activate AMPK, and block tumor cell growth in animal models.
14325
23.04.13
CP 690,550
A JAK inhibitor
CP 690,550 is a potent, cell-permeable inhibitor of all JAK isoforms (IC50 = 6.1, 12, and 8.0 nM for JAK1, JAK2, and JAK3, respectively). Originally recognized as a JAK3 blocker, it was found to be effective in preventing organ allograft rejection. CP 690,550 is now used to ameliorate inflammatory or autoimmune components of a host of diseases, including rheumatoid arthritis and ulcerative colitis.
11598
23.04.13
Genistin
A natural isoflavone
Genistin is a natural isoflavone isolated from legumes, including soy and kudzu. It is a phytoestrogen, as it stimulates the growth of estrogen-dependent human breast cancer cells in vivo. Like other isoflavones, genistin promotes the proliferation of bone marrow stromal cells and osteoblasts and suppresses bone turnover. It also increases bone formation in collagen matrix in vivo.
14174
23.04.13
Glyburide (potassium salt)
K+ channel inhibitor which stimulates insulin secretion
Glyburide is a sulfonylurea compound which acts as an inhibitor of ATP-dependent inwardly-rectifying K+ channels (IC50 = 4.3 nM). Through this action, glyburide stimulates insulin secretion from beta cells. Independent of its effects on potassium channels, glyburide (200 μM) inhibits cryopyrin inflammasome activation, preventing IL-1β and IL-18 processing and secretion. It also has anti-leishmanial activity.
15009
23.04.13
Glycitin
A natural isoflavone
Glycitin is a natural isoflavone isolated from legumes, including soy and kudzu. Like other isoflavones, glycitin promotes the proliferation of bone marrow stromal cells and osteoblasts and suppresses bone turnover.
14161
23.04.13
Irinotecan (hydrochloride)
A potent inhibitor of DNA topoisomerase I
Irinotecan, a derivative of the alkaloid camptothecin (Item No. 11694), functions as a prodrug that is converted by tissue carboxylesterase to 7-ethyl-10-hydroxycamptothecin, a potent inhibitor of DNA topoisomerase I. Its action is terminated by glucuronidation by UDP glucuronosyl transferase 1A1. Irinotecan demonstrates a broad spectrum of antitumor activity against metastatic colorectal cancer, small cell lung cancer, and several other solid tumors and has proven useful in radiation treatment of tumors by sensitizing tissue to radiation damage.
14180
23.04.13
Isopropyl dodec-11-enylfluorophosphonate
A dual inhibitor of CB1 and FAAH
Isopropyl dodec-11-enylfluorophosphonate is an organophosphorus ester that antagonizes the central cannabinoid (CB1) receptor and inhibits FAAH with similar potencies (IC50s = 2 nM). At 30 mg/kg, this compound inhibits 99% of the brain neuropathy target esterase-lysophospholipase, which is attributed to causing delayed toxicity in mice.
11613
23.04.13
Methylprednisolone
A synthetic glucocorticoid
Methylprednisolone is a 6α-methyl derivative of prednisolone, a variation which reduces its binding to corticosteroid-binding globulin and increases penetration into target tissues. It alters gene expression, like prednisolone, through both the glucocorticoid and mineralocorticoid receptors.
15013
23.04.13
Tigecycline
A glycylcycline antibiotic
Tigecycline is a glycylcycline antibiotic that binds to the bacterial 30S ribosome, blocking the entry of transfer RNA, which halts protein synthesis and thus limits bacterial growth. It has a broad spectrum of activity against many Gram-positive, Gram-negative, and anaerobic organisms, including many multidrug-resistant strains.
15026
23.04.13
Topotecan (hydrochloride)
A potent inhibitor of DNA topoisomerase I
Topotecan is a water soluble analog of the alkaloid camptothecin that potently inhibits DNA topoisomerase I. It induces cytoxicity and DNA damage in human HT-29 colon adenocarcinoma cells with IC50 values of 33 nM and 0.28 μM, respectively. Topotecan demonstrates a broad spectrum of antitumor activity against a variety of other tumors including ovarian cancer, cervical cancer, neuroblastoma, brainstem glioma, and Ewing’s sarcoma.
14129
18.04.13
Doxorubicin (hydrochloride)
An anthracycline antitumor antibiotic
Doxorubicin is an anthracycline antitumor antibiotic that inhibits DNA topoisomerase II by inducing double-stranded DNA breaks. By intercalating within DNA, doxorubicin inhibits nucleic acid synthesis and induces apoptosis by inducing the accumulation of the p53 tumor suppressor protein.
15007
18.04.13
Linezolid
An antibiotic active against Gram-positive bacteria
Linezolid is a synthetic oxazolidinone antibiotic active against a wide range of Gram-positive bacteria, including resistant strains of several species, such as MRSA, penicillin-resistant pneumococci, vancomycin-resistant enterococci, many different streptococci, various anaerobic bacteria, and several mycobacteria. Linezolid inhibits protein synthesis by binding to domain V of the 23S ribosomal RNA of the 50S subunit of bacterial ribosomes.
15012
18.04.13
OC000459
A potent, selective DP2 antagonist
OC000459 is a potent, selective DP2 antagonist that displaces [3H]prostaglandin D2 ([3H]PGD2) from human recombinant DP2 receptors (Ki = 13 nM), rat recombinant DP2 receptors (Ki = 3 nM), and human native DP2 (Ki = 4 nM; Th2 cell membranes) without interfering with the ligand binding properties of other prostanoid receptors, including PGE1–4, DP1, TP, PGI2, and PGF. OC000459 inhibits chemotaxis and cytokine production of human Th2 lymphocytes with IC50 values of 28 and 19 nM, respectively, and competitively antagonizes eosinophil shape change responses induced by PGD2 in both isolated human leukocytes (pKB = 7.9) and human whole blood (pKB = 7.5). OC000459 was shown to inhibit blood eosinophilia in rats induced by 13,14-dihydro-15-keto PGD2 (Item No. 12610) (ED50 = 0.04 mg/kg) and airway eosinophilia in guinea pigs in response to an aerosol of 13,14-dihydro-15-keto PGD2 (ED50 = 0.01 mg/kg).
12027
18.04.13
PF-05274857 (hydrochloride)
An antagonist of Smoothened
PF-05274857 is an antagonist which binds Smo (Ki = 4.6 nM), blocking Gli1 transcription in cells stimulated with Shh (IC50 = 2.7 nM). When administered orally, it distributes through plasma to skin and tumor and remains metabolically stable. PF-05274857 also penetrates the blood-brain barrier and inhibits Smo activity in the brain.
15022
17.04.13
Bazedoxifene acetate
A selective estrogen receptor modulator
Bazedoxifene acetate is a third generation selective estrogen receptor modulator (SERM). It is an indole-based ER ligand that binds to both ERα (IC50 = 26 nM) and ERβ (IC50 = 99 nM). Bazedoxifene actetate antagonizes 17β-estradiol-dependent MCF-7 and T47D breast cancer cell proliferation in vitro as well as hormone-independent growth of MCF-7:5C cells that are resistant to long-term estrogen deprivation (80% reduction with 10 nM). It has been shown to arrest cell cycling by downregulating cyclin D1 and ERα.
15005
17.04.13
PF-04708671
A specific, cell-permeable inhibitor of S6K1
PF-04708671 is a specific, cell-permeable inhibitor of S6K1 (IC50 = 160 nM). It does not inhibit S6K2, MSK, or RSK, or many other unrelated kinases, under conditions in which it inhibits S6K1 activity. It is useful in evaluating the role of S6K1 and, indirectly, mTORC1, in cell signaling.
15018
17.04.13
PF-04981517
A potent, selective inhibitor of CYP3A4
PF-04981517 is a potent, time-dependent inhibitor of CYP3A4 (IC50 = 30 nM). It is less effective against CYP3A5 and CYP3A7 (IC50s = 17 and 70 μM, respectively). PF-04981517 will be useful for understanding the relative roles of CYP3A4 and CYP3A5 in drug metabolism.
15019
17.04.13
Prazosin (hydrochloride)
An α1-adrenergic receptor antagonist
Prazosin is an antihypertensive agent that blocks postsynaptic α1-adrenergic receptors in the periphery (IC50 = 0.20 nM in dog aorta) and is capable of crossing the blood-brain barrier, decreasing sympathetic outflow in the brain (IC50 = 1.7 nM in rat brain). Prazosin is also a potent antagonist at the melatonin MT3 receptor (Ki = 10.2 - 12.4 nM; IC50 = 7.8 nM in hamster).
15023
17.04.13
Sulfasalazine
A prodrug of 5-aminosalicylic acid
Sulfasalazine is a prodrug of the anti-inflammatory agent 5-aminosalicylic acid that is covalently linked to the antibiotic sulfapyridine by an azo bond. This bond is rapidly cleaved by bacteria in the terminal ileum and colon, thus releasing the active anti-inflammatory component. It has long been used in treatment of inflammatory bowel disease and rheumatoid arthritis because of its ability to induce T lymphocyte apoptosis, modulate inflammatory mediators from both cyclooxygenase/5-lipoxygenase pathways and NF-κB signaling pathways, attenuate transcription of proinflammatory cytokines, and activate PPARγ.
15025
17.04.13
Ziprasidone (hydrochloride hydrate)
A combined serotonin and dopamine receptor antagonist
Ziprasidone is the hydrochloride salt of a benzisothiazolylpiperazine analog structurally related to the atypical antipsychotic drug tiospirone that antagonizes both central serotonin 5-HT2A (Ki = 0.42 nM) and dopamine D2 (Ki = 4.8 nM) receptors. It is also a potent agonist at 5-HT1A receptors (Ki = 3.4 nM), increasing cortical dopamine release which may offset negative effects associated with dopamine D2 antagonism, and an inverse agonist at 5-HT1B and 5-HT1D receptors (pKis = 8.8 and 8.6, respectively).
15031
16.04.13
DPQ
An inhibitor of poly(ADP-ribose) polymerases
DPQ is a potent inhibitor of PARPs, inhibiting PARP-1 with an IC50 value of 40 nM. It is approximately 10-fold less potent against PARP-2. DPQ can be used in either cells or in animals.
14450
16.04.13
Miglitol
An inhibitor of α-glucosidases
Miglitol is a pseudo-carbohydrate which inhibits α-glucosidases, inhibiting lysosomal α-glucosidase, sucrase, maltase, and isomaltase (IC50s = 0.35, 0.11, 1.3, and 1.2 μM, respectively). It also inhibits maltase-glucoamylase (IC50 = 1.0 μM). Miglitol can be used to prevent postprandial hyperglycemia associated with diabetes without cardiovascular complications.
15014
16.04.13
PF-04418948
An orally active, potent, selective EP2 receptor antagonist
PF-04418948 is an orally active, potent, and selective EP2 receptor antagonist (IC50 = 16 nM). It is over a thousand-fold less active at other prostanoid receptors, including other EP receptors. PF-04418948 can be used in cells and tissues. In rats, it significantly reduces the effects of the EP2-selective agonist butaprost on cutaneous blood flow when given orally.
15016
16.04.13
PJ-34 (hydrochloride)
An inhibitor of poly (ADP-ribose) polymerases
PJ-34 is an inhibitor of PARPs which can be used in cells or in animals. It binds and inhibits the PARP tankyrase1 (IC50 = 1 μM). PJ-34 also inhibits matrix metalloproteinase-2 when used at higher concentrations (IC50 = 56 μM).
14440
15.04.13
Bosutinib
A potent inhibitor of Src and Abl kinases
Bosutinib is best known as a potent dual inhibitor of c-Src and Abl (IC50 = 1.2 and 1.0 nM, respectively). Consistent with this action, bosutinib can be effective in regulating tumor growth and differentiation. Bosutinib also inhibits, at nanomolar concentrations, other members of the Src family (e.g., Yes, Fgr, Lck, Fyn), as well as members of the TEC family, and certain other kinases. These actions extend the usefulness of this compound to cancers beyond those involving Src and Abl.
12030
15.04.13
Jasplakinolide
A binder and modulator of F-actin
Jasplakinolide is a natural macrocyclic peptide first isolated from a marine sponge. It potently inhibits the proliferation of PC3 prostate carcinoma cells (IC50 = 35 nM) by binding F-actin (KD = 15 nM). This binding of jasplakinolide to actin, which is competitive with phalloidin, stabilizes actin filaments in vitro but disrupts actin filaments and induces irregular polymerization of monomeric actin in vivo. This compound is used to investigate the role of actin in diverse cellular roles, such as motility, transport, and development.
11705
15.04.13
β-Glycerophosphate (sodium salt hydrate)
A potent inhibitor of phosphatase
β-Glycerophosphate is a protein phosphatase inhibitor that acts as a phosphate group donor in matrix mineralization studies. It promotes bone matrix mineralization when delivered to osteoblasts by providing a source of phosphate ions. β-Glycerophosphate (10 mM) accelerates calcification of cultured vascular smooth muscle cells through an alkaline phosphatase-related mechanism.
14405
12.04.13
(±)-para-Octopamine (hydrochloride)
An endogenous biogenic amine
(±)-para-Octopamine ((±)-p-Octopamine) is an endogenous biogenic amine commonly found in invertebrates. Structurally similar to norepinephrine, (±)-p-octopamine activates adrenergic-like receptors and evokes effects, in invertebrates, that parallel those of norepinephrine and epinephrine in mammals. In humans, (±)-p-octopamine is considered a trace amine which may interfere with aminergic pathways as well as signal through trace amine-associated receptors.
14279
12.04.13
Pseurotin A
A fungal secondary metabolite
Pseurotin A is a secondary metabolite produced by Aspergillus and other fungi. Its expression is induced in response to hypoxia. Pseurotin A has been shown to inhibit IgE production by mouse B cells in culture (IC50 = 3.6 μM) and dose-dependently (0.4-25 μg/ml) stimulate neuritogenic activity in rat pheochromocytoma PC12 cells. It also demonstrates nematicidal activity at 300 μg/ml.
14441
12.04.13
Ruthenium Red
A polycationic dye that blocks Ca2+ release
Ruthenium red is a polycationic dye that inhibits sarcoplasmic reticulum Ca2+ release, blocks Ca2+ uptake and release from mitochondria, and prevents Ca2+ release from ryanodine-sensitive intracellular stores in skeletal and cardiac muscle (Kis = 16 nm - 5.9 μM, depending on Ca2+ concentration). Additionally, ruthenium red binds to anionic sites of cellular components, predominantly to surface glycoconjugates, and can be used as a marker of negative binding sites related to cellular transport, barrier, or receptor functions.
14339
11.04.13
1,5-Isoquinolinediol
An inhibitor of poly(ADP-ribose) polymerases
1,5-Isoquinolinediol is an inhibitor of poly(ADP-ribose) synthetase (PARP1; IC50 = 0.39 μM). It has been used to study the role of PARP1 in both DNA repair and oxidant stress-induced cell death. This compound can be used with cells in culture and in animals.
14438
11.04.13
bpV(HOpic) (potassium salt)
A PTEN inhibitor
bpV(HOpic) is a bisperoxovanadium (bpV) compound that inhibits several different protein tyrosine phosphatases (PTPs), with selectivity for PTEN (IC50 = 14 nM). It also inhibits the vascular endothelial PTP, PTP-β (IC50 = 4.9 μM), and PTP-1βB (IC50 = 25.3 μM). At 15 μM, bpV(HOpic) has been shown to protect against stimulated ischemia-reperfusion injury in vitro by decreasing apoptosis and improving cell viability through the upregulation of the PI3K/Akt/eNOS/ERK prosurvival pathway.
14433
11.04.13
bpV(pic) (potassium hydrate)
A PTEN inhibitor
bpV(pic) is a bisperoxovanadium (bpV) compound that inhibits several different protein tyrosine phosphatases (PTPs), with selectivity for PTEN (IC50 = 31 nM). It also inhibits the vascular endothelial PTP, PTP-β (IC50 = 12.7 μM), and PTP-1βB (IC50 = 61 μM). bpV(pic) is also known to be an insulin mimetic capable of activating the insulin receptor kinase of cultured hepatoma cells, stimulating lipogenesis in adipocytes, and inhibiting the dephosphorylation of autophosphorylated insulin receptors and epidermal growth factor receptors of rat liver endosomes.
14434
11.04.13
Chetomin
An inhibitor of HIF signaling
Chetomin is a natural product isolated from Chaetomium species which has antibacterial and antifungal properties. It is a small molecule inhibitor of hypoxia-inducible factor (HIF) signaling, disrupting the binding of HIF-1α and HIF-2α to p300 at low nanomolar concentrations. Chetomin effectively attenuates the HIF pathway both in cells and in vivo, in mice. It inhibits HIF-dependant signaling, cell growth, and tumor growth in cancer cells and xenografts.
14437
11.04.13
Clofarabine
A nucleoside analog used in the treatment of leukemia
Clofarabine is a nucleoside analog that inhibits ribonucleotide reductase and DNA polymerase-α (IC50s = 65 and 3.9 nM, respectively) and is cytotoxic to K562 myelogenous leukemia cells (IC50 = 5 nM). It induces apoptosis in primary chronic lymphocytic leukemia cells by directly altering mitochondrial transmembrane potential. Clofarabine demonstrates growth inhibition and cytotoxic activity in a variety of leukemias and solid tumors.
14125
11.04.13
Fludarabine
A nucleoside analog used in the treatment of leukemia
Fludarabine is an adenosine deaminase resistant analog of 9-β-D-arabinofuranosyladenine (ara-A) that disrupts ribonucleotide reductase and DNA polymerase in blood cells. It exhibits antiproliferative activity (IC50 = 1.54 μM in an RPMI8226 myeloma cell line) and triggers apoptosis through increasing Bax and decreasing Bid, XIAP, and survivin expression. Fludarabine is effective in a number of animal tumor systems including LI210 leukemia, CD8F mammary adenocarcinoma, P388 leukemia, and human LX-1 lung tumor xenograft and displays anticancer activity against human hematological malignancies in vivo.
14128
11.04.13
Obscurolide A1
A phosphodiesterase inhibitor
Obscurolide A1 is a natural butyrolactone isolated from S. viridochromogenes. It inhibits calcium/calmodulin-dependent phosphodiesterase from bovine brain, presumably PDE1 (IC50 = 15 mM).
14439
10.04.13
Asperlactone
An antibiotic with nematicidal, insecticidal, antibacterial, and antifungal activity
Asperlactone is a nematicidal, insecticidal, antibacterial, and antifungal polyketide metabolite produced from A. westerdijkiae.
14435
10.04.13
Borrelidin
An anti-angiogenic antibiotic
Borrelidin is a secondary metabolite produced by Streptomyces and other bacteria. It displays potent anti-angiogenic activity, preventing tube formation in rat aorta explants (IC50 = 0.8 nM) and inducing apoptosis in endothelial cells. Borrelidin also alters the splicing of VEGF mRNA, producing an anti-angiogenic isoform of the growth factor. It has long been known as a powerful inhibitor of both eukaryotic and bacterial threonyl tRNA synthetase. Borrelidin is also an effective anti-malarial drug, as it kills P. falciparum with an IC50 value of 1.8 nM. At higher doses, it inhibits cyclin-dependent kinase in yeast (IC50 = 24 μM), resulting in growth arrest in the G1 phase.
14436
10.04.13
Daunorubicin (hydrochloride)
Antitumor antibiotic used in the treatment of acute myeloid leukemias
Daunorubicin is an antitumor antibiotic widely used in the treatment of acute myeloid leukemias (AMLs). At 0.2-1μM, daunorubicin induces apoptosis in mature monocytic U937 and myelocytic HL-60 AML cells. However, immature AML cells (CD 34+-KG1a, -KG1, or -HEL cells) appear resistant to apoptosis at similar concentrations. In mature AML cells, daunorubicin has been shown to trigger a ROS-dependent sphingomyelin-ceramide pathway that activates the MEKK1-SEK1-JNK cascade leading to enhanced DNA binding activity of the transcription factor AP-1.
14159
10.04.13
Interleukin-5 (mouse) EIA Kit
Enzyme immunometric assay for the measurement of mouse IL-5
Limit of detection: 15.6 pg/ml · Interleukin-5 (IL-5) is a TH2 cytokine produced primarily by activated TH2 cells, and also by mast cells, natural killer (NK) cells, and natural helper cells. Mouse IL-5 induces the terminal differentiation and immunoglobulin secretion from B cells and is required for the differentiation and proliferation of eosinophils. Cayman’s IL-5 (mouse) EIA Kit is an immunometric (i.e., sandwich) EIA that permits IL-5 measurements within the range of 0-1,000 pg/ml, with a limit of detection of 15.6 pg/ml.
500880
08.04.13
Aldehyde Dehydrogenase Activity Assay Kit
For the detection of ALDH activity in tissue homogenates, cell culture samples, and purified ALDH preparations
Limit of detection: 0.4 U/ml (±0.1 U/ml) ALDH · Aldehyde dehydrogenases (ALDHs) represent a group of enzymes that oxidize a wide range of endogenous and exogenous aldehydes to their corresponding carboxylic acids, which affect both developmental and toxicological functions. Pharmacological inhibitors or activators of ALDH activity have been developed to examine the metabolism of alcohol as well as a number of pathological conditions, including cancer, Type II hyperprolinemia, Sjögren-Larsson Syndrome, Parkinson’s Disease, Cardiac Disease, and hyperammonemia. Cayman’s Aldehyde Dehydrogenase Assay provides a fluorescence-based method for detecting ALDH activity in tissue homogenates, cell culture samples, and purified ALDH preparations. In the assay, ALDH catalyzes the oxidation of acetaldehyde to acetic acid, along with the concomitant reduction of NAD+ to NADH. NADH reacts with the fluorometric developer to yield a highly fluorescent product which can be analyzed with an excitation wavelength of 530-540 nm and an emission wavelength of 585-595 nm.
700800
08.04.13
Clindamycin
An antibiotic of the lincosamide class
Clindamycin is an antibiotic in the lincosamide class which binds the bacterial 50S ribosomal subunit and interferes with protein synthesis. Evidence suggests that clindamycin is particularly effective against anaerobes and is commonly used against Gram positive bacteria. It is used for serious infections and in the prevention of emerging infections in burns. Clindamycin is also effective against P. falciparum and is used as an antimalarial, either alone or in combination therapy.
15006
08.04.13
PF-03814735
An inhibitor of Aurora A and B kinases
PF-03814735 is a reversible inhibitor of both Aurora A and Aurora B kinases with IC50 values of 0.8 and 5 nM, respectively, in in vitro activity assays. PF-03814735 also inhibits the kinases Flt1, FAK, TrkA, Met, and FGFR1 with IC50 values of 10, 22, 30, 100, and 100 nM, respectively. PF-03814735 inhibits cell proliferation of HCT-116, HL-60, A549, and H125 tumor cell lines with IC50 values ranging from 42-150 nM and shows in vivo efficacy in an HCT-116 tumor xenograft mouse model. PF-03814735 has been shown to be particularly sensitive towards inhibiting the growth of small cell lung cancer cell lines and other tumors driven by the Myc family genes.
15015
08.04.13
PF-04691502
A dual inhibitor of PI3K and mTOR
PF-04691502 is a potent, ATP competitive, dual inhibitor of PI3K and mTOR. It selectively inhibits human PI3K isoforms α, β, δ, and γ (Kis = 1.8, 2.1, 1.6, and 1.9 nM, respectively) and human mTOR (Ki = 16 nM) without significantly inhibiting a panel of more than 80 related protein kinases at concentrations up to 10 μM. PF-04691502 inhibits cell proliferation of BT20 (breast), SKOV3 (ovarian), and U87MG (glioblastoma) cancer cells with IC50 values of 313, 188, and 179 nM, respectively, and shows good in vivo efficacy in U87MG, SKOV3, and four separate non-small cell lung cancer xenograft mouse models. PF-04691502 has been used to inhibit activation of PI3K and mTOR effector kinases and prevent a p27-dependent increase in cell motility and invasion in a highly bone-metastatic model of breast cancer.
15017
08.04.13
Torcetrapib
An inhibitor of CETP activity
Torcetrapib is an inhibitor of CETP activity (IC50 = 50 nM) that raises HDL cholesterol and reduces LDL cholesterol levels by forming a nonproductive complex between CETP and HDL. Although torcetrapib produced consistent antiatherogenic effects in rabbits, clinical trials of torcetrapib were terminated early due to deleterious hypertensive effects. PDGFR, HGFR (c-Met), IL-2 receptor, and ErbB1- tyrosine kinase have subsequently been identified as direct off-targets of this compound.
15028
04.04.13
Alsterpaullone
A dual CDK and GSK-3 inhibitor
Alsterpaullone is a derivative of kenpaullone (Item No. 10010239), an ATP-competitive inhibitor of several cyclin-dependent kinases (CDKs) as well as glycogen synthase kinase 3β (GSK-3β). With slightly improved potency over kenpaullone, alsterpaullone selectively inhibits CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E, CDK5/p25, and GSK-3α/β with IC50 values of 35, 15, 200, 40, and 4 nM, respectively. Alsterpaullone has been used to inhibit the cytosolic degradation of β-catenin to alter the canonical Wnt signaling pathway in primary axis patterning, to reduce tau phosphorylation in an effort to modify neuropathological events associated with Alzheimer’s disease, and to alter cell proliferation or protein expression in various diseases.
14428
04.04.13
(+)-Aphidicolin
A cell-permeable, reversible inhibitor of DNA polymerases
(+)-Aphidicolin is a natural tetracyclic diterpene first isolated from the fungus C. aphidicola and shown to have antiviral activity against herpes simplex. In eukaryotic cells, it is a cell-permeable, reversible inhibitor of DNA replication, specifically blocking the activity of DNA polymerases α, δ, and ε when used at low micromolar levels. Aphidicolin can be used, at 3 μM, to arrest cells in G1/S phase or to increase gene amplification frequency.
14007
04.04.13
Docosaenoyl Ethanolamide
An endocannabinoid
Docosaenoyl ethanolamide is a member of the family of fatty N-acyl ethanolamines collectively called endocannabinoids. This long-chain ethanolamine has been detected at relatively high levels in rat cerebrospinal fluid and has been used to examine the function of voltage-dependent Ca2+ channels in skeletal muscle membranes.
9001745
04.04.13
Nervonoyl Ethanolamide
An endocannabinoid
Nervonoyl ethanolamide is a member of the family of fatty N-acyl ethanolamines collectively called endocannabinoids. The relative importance of this ethanolamine metabolite has not been determined.
9001746
03.04.13
Indirubin
A natural inhibitor of GSK3 and CDK isoforms
Indirubin is a natural product originally extracted from roots and leaves of the Indigo plant (I. tinctoria) used in traditional Chinese medicine for anti-inflammatory, anti-tumor, and neuroprotective effects. Indirubin inhibits glycogen synthase kinase-3 (IC50 = 2.5 μM) and cyclin-dependent kinases 1 and 5 (IC50 = 10 μM for both isoforms).
14155
03.04.13
Tricosanoyl Ethanolamide
An endocannabinoid
Tricosanoyl ethanolamide is a member of the family of fatty N-acyl ethanolamines collectively called endocannabinoids. The relative importance of this ethanolamine metabolite has yet to be determined.
9001743
03.04.13
Valsartan
An angiotensin II receptor antagonist
Valsartan is a nonpeptide angiotensin II receptor antagonist which selectively and insurmountably inhibits the angiotensin II AT1 receptor subtype (IC50 = 2.7 nM). It has about 20,000-fold higher affinity for AT1 over AT2 and, unlike some other AT receptor blockers, does not alter PPARγ activity or show significant drug interactions. Valsartan, alone or in combination therapy, has significant cardioprotective effects.
14178
03.04.13
γ-Linolenoyl Ethanolamide
An endocannabinoid
γ-Linolenoyl ethanolamide is a member of the family of fatty N-acyl ethanolamines collectively called endocannabinoids. The relative importance of this ethanolamine metabolite has yet to be determined.
9001747
02.04.13
Febuxostat
A potent inhibitor of xanthine oxidoreductase
Febuxostat is an antihyperuricemic nonpurine inhibitor of both the oxidized and reduced forms of xanthine oxidase. It is 10-30 times more potent than the hypoxanthine analog allopurinol (Kis = 0.7 nM versus 0.7 μM, respectively). In various clinical trials, 40-120 mg/day febuxostat was proven effective in lowering serum urate levels when administered to manage hyperuricemia in patients with gout.
14127
02.04.13
Pemetrexed (sodium salt hydrate)
A multi-targeted antifolate with antitumor activity
Pemetrexed is pyrrotopyrimidine-based, multi-targeted antifolate with broad in vivo antitumor activity. Originally identified as a highly efficient substrate for folylpolyglutamate synthase, pemetrexed potently inhibits multiple folate-dependent enzymes involved in both purine and pyrimidine synthesis including thymidylate synthase (Ki = 109 nM), dihydrofolate reductase (Ki = 7 nM), glycinamide ribonucleotide formyltransferase (Ki = 9.3 μM), and aminoimidazole carboxamide ribonucleotide formyltransferase (Ki = 3.6 μM). Its antiproliferative activity has been demonstrated in a wide variety of solid tumors, including non-small cell lung, breast, mesothelioma, colorectal, pancreatic, gastric, bladder, cervix, and head and neck.
14269
01.04.13
Catharanthine
A plant alkaloid used to synthesize anticancer antibiotics
Catharanthine is a precursor of the vinblastine and vincristine group of alkaloids found in the Vinca plant, C. roseus that have been used widely in chemotherapy regimens. It is biologically active in synergy with similar indole alkaloids and can be used as starting material for the synthesis of vinblastine and vincristine.
11695
01.04.13
Floxuridine
A prodrug of 5-fluorouracil
Floxuridine is a prodrug that is rapidly catabolized in vivo to 5-fluorouracil when administered by rapid injection. In addition, floxuridine inhibits thymidylate synthase (EC50 = 0.6 nM), interfering with DNA synthesis. It has been used to treat various cancers, particularly metastases to the liver.
14154
01.04.13
PD 150606
An inhibitor of calpains
PD 150606 is a selective, cell-permeable inhibitor of calpains (Ki = 0.21 μM for μ-calpain (calpain-1) and 0.37 μM for m-calpain (calpain-2)). PD 150606 is commonly used to elucidate the roles for calpains in cell function, particularly in how they relate to apoptosis.
13859
27.03.13
A-769662
A direct activator of AMPK
A-769662 is a small molecule thienopyridone that activates AMPK directly in cell-free assays (EC50 = 116 nM) and intact cells by allosterically activating AMPK and inhibiting its dephosphorylation on Thr172. A-769662 specifically activates β1 subunit-containing AMPK heterotrimers, and its effects are independent of kinases upstream of AMPK. A-769662 has been used to stimulate CYP450-mediated fatty acid oxidation, inhibit adipocyte differentiation, explore glucose uptake in skeletal muscle, and promote endothelial cell survival during metabolic stress.
11900
27.03.13
Acyclovir
A selective, antiviral guanosine analog
Acyclovir is a guanosine analog with antiviral activity in vitro against the herpes simplex viruses, varicella zoster virus, Epstein-Barr virus, cytomegalovirus, and human herpes virus 6 (ID50s = 0.1 - 63.1 μM). Acyclovir differs from most nucleoside analogs in that it contains only a partial nucleoside structure with an acyclic side chain. It diffuses freely into cells and is selectively converted into acyclo-guanosine monophosphate by a virus-specific thymidine kinase. During DNA replication, the phosphorylated form of acyclovir is preferentially incorporated into viral DNA, resulting in premature chain termination and inhibition of further activity of DNA polymerase.
14160
27.03.13
Torin 2
Selective inhibitor of mTOR
Torin 2 is a potent and selective inhibitor of cellular mTOR activity (EC50 = 0.3 nM). It shows more than 800-fold selectivity for mTOR over PI3K (EC50 = 200 nM) and greater than 100-fold binding selectivity relative to 440 other protein kinases. Torin 2 has significantly improved bioavailability (54%), metabolic stability, and plasma exposure compared to Torin 1 (Item No. 10997).
14185
26.03.13
Bicalutamide
A non-steroidal antiandrogen
Bicalutamide is a non-steroidal androgen receptor antagonist that binds the androgen receptor (Ki = 12.5 μM; IC50 = 1.2 μM), preventing its activation and subsequent upregulation of androgen responsive genes by androgenic hormones. Bicalutamide is frequently used to examine the role of androgen receptor inactivation in the proliferation of prostate cancer cells and has served as a molecular template for the design and structural optimization of more selective androgen receptor modulators for androgen therapy.
14250
26.03.13
JC-1
An indicator dye of mitochondrial transmembrane potential
JC-1 is a membrane-permeable cationic dye that is used to study mitochondrial integrity in the context of cellular apoptosis. It selectively enters mitochondria and changes fluorescence characteristics with alteration in mitochondrial transmembrane potential (ΔΨm). In healthy cells with a high mitochondrial ΔΨm, JC-1 forms complexes known as J-aggregates, which fluoresce red/orange and may be detected using FL2 settings by flow cytometry. A drop in ΔΨm, a very early event in apoptosis, results in JC-1 monomers, which fluoresce green (FL1 settings on flow cytometers). JC-1 may also be used with fluorescent microscopes or plate readers, using excitation at 520-570 nm and emission at 570-610 nm for J-aggregates and excitation at 485 nm and emission at 535 nm for monomers.
15003
26.03.13
Lignoceroyl Ethanolamide
An endocannabinoid
Lignoceroyl ethanolamide is a member of the family of fatty N-acyl ethanolamines collectively called endocannabinoids. Whereas lignoceric acid has been detected at relatively high levels in rat cerebrospinal fluid, the specific role and relative importance of its ethanolamine metabolite have not been determined.
9001744
26.03.13
Myristoyl Ethanolamide
An endocannabinoid
Myristoyl ethanolamide is a member of the family of fatty N-acyl ethanolamines collectively called endocannabinoids. Myristic acid is typically detected at low levels in rat cerebrospinal fluid, however the specific role and relative importance of its ethanolamine metabolite have not been yet determined.
9001742
26.03.13
Pentadecanoyl Ethanolamide
An endocannabinoid
Pentadecanoyl ethanolamide is a member of the family of fatty N-acyl ethanolamines collectively called endocannabinoids. The specific role and relative importance of this ethanolamine metabolite have not been determined.
9001740
21.03.13
SMN tudor domain (human recombinant)
Source: recombinant N-terminal GST-tagged protein expressed in E. coli · Mr: 42.6 kDa ·
14136
20.03.13
Flumazenil
A GABAA-benzodiazepine receptor antagonist
Flumazenil is an imidazobenzodiazepine derivative that competitively inhibits benzodiazepine binding to GABAA receptors with an IC50 value of 2 nM. Flumazenil is non-selective for α1, α2, α3, or α5 subunit-containing GABAA receptors and antagonizes the actions of benzodiazepines on the central nervous system without producing the behavioral or neurological effects typical of the benzodiazepines. Flumazenil has been used to reverse sedation induced by benzodiazepine drugs and has been found to be effective in the treatment of benzodiazepine overdose or withdrawal.
14252
20.03.13
IDH1 (human recombinant)
Source: recombinant C-terminal His-tagged protein expressed in E. coli · Mr: 47.9 kDa ·
14131
20.03.13
IDH1 R132H mutant (human recombinant)
Source: recombinant C-terminal His-tagged protein expressed in E. coli · Mr: 47.9 kDa ·
14132
18.03.13
EBPC
A potent aldose reductase inhibitor
EBPC is a potent, selective inhibitor of aldose reductase with an IC50 value of 47 nM in vitro. Through its regulation of glucose metabolism, EBPC has been used to improve the cytotoxic effects of the anticancer agents doxorubicin and cisplatin in HeLa cervical carcinoma cells. EBPC also inhibits prostaglandin F2α (PGF2α) and PGE2 production in human endometrial cells with an EC50 value of 10 μM.
14183
18.03.13
OAC3
An Oct4-activating compound
OAC3 is an Oct-4-activating compound which activates expression through the Oct-4 gene promoter. In cells expressing Oct-4 with Sox2, Klf4, and c-Myc, OAC3 (1 μM) enhances reprogramming efficiency by increasing the rate of production of induced pluripotent stem cells from embryonic fibroblasts.
14104
18.03.13
Prostaglandin D2 Ethanolamide-d4
An internal standard for the quantification of PGD2-EA
Prostaglandin D2 ethanolamide (PGD2-EA)-d4 contains four deuterium atoms. It is intended for use as an internal standard for the quantification of PGD2-EA by GC- or LC-mass spectrometry.
9001413
18.03.13
SL 0101-1
A selective inhibitor of RSK
SL 0101-1 is a kaempferol glycoside, isolated from the tropical plant F. refracta, that selectively inhibits RSK2 with an IC50 value of 89 nM (Ki = 1 μM) without interfering with upstream activators of RSK, including ERK, MEK, EGFR, and PKC. At 100 μM, SL 0101-1 inhibits the proliferation of MCF-7 breast cancer cells, arresting cells in the G1 phase of the cell cycle. SL 0101-1 has been used to characterize the intracellular signaling events associated with angiotensin II-induced tyrosine kinase activation with a concentration of 30 μM attenuating angiotensin II-induced cell proliferation.
11704
15.03.13
GPR12 (C-Term) Polyclonal Antibody
Antigen: human GPR12 amino acids 323-334 · Host: rabbit · Application(s): FC and ICC ·
14266
15.03.13
GPR12 (N-Term) Polyclonal Antibody
Antigen: human GPR12 amino acids 2-16 · Host: rabbit · Application(s): FC and ICC ·
14267
15.03.13
OAC2
An Oct4-activating compound
OAC2 is an Oct-4-activating compound which activates expression through the Oct-4 gene promoter. In cells expressing Oct-4 with Sox2, Klf4, and c-Myc, OAC2 (1 μM) enhances reprogramming efficiency by increasing the rate of production of induced pluripotent stem cells (iPSCs) from embryonic fibroblasts. The iPSCs developed using OAC2 retain the capacity for pluripotent differentiation, whether evaluated in vitro or in vivo.
14103
15.03.13
Puerarin
A natural isoflavonoid
Puerarin is a natural isoflavone isolated from plants of the genus Pueraria used in traditional Chinese herbal medicine. It is biotransformed by intestinal bacteria to give the phytoestrogens daidzein (Item No. 10005166) and equol (Item No. 13184), resulting in antithrombotic, antiallergic, and other salutary effects. When given intraperitoneally, puerarin evokes diverse responses by modulating serotonin receptors. This compound also suppresses lipopolysaccharide-mediated activation of NF-κB in RAW 264.6 macrophages when given at 20-40 μM.
14175
14.03.13
GPR120 (C-Term) Polyclonal Antibody
Antigen: human GPR120 amino acids 364-375 · Host: rabbit · Application(s): ELISA, ICC, and WB ·
14265
14.03.13
KN-93 (hydrochloride)
A selective inhibitor of Ca2+/calmodulin-dependent kinase II
KN-93 is a selective inhibitor of Ca2+/calmodulin-dependent kinase II (CaMKII), competitively blocking CaM binding to the kinase (Ki = 370 nM). It does not affect the activities of PKA, PKC, MLCK, or Ca2+-phosphodiesterase. It inhibits histamine-induced aminopyrine uptake in parietal cells (IC50 = 300 nM). More recently, KN-93 has been used to implicate roles for CaMKII in Ca2+-induced Ca2+ release in cardiac myocytes, constitutive phosphorylation of 5-lipoxygenase in 3T3 cells, and Ca2+-dependent activation of HIF-1α in colon cancer cells.
13864
14.03.13
Oxygen Consumption Rate Assay Kit (MitoXpress® - Xtra HS Method)
For the measurement of oxygen consumption rate in living cells
The oxygen consumption rate (OCR) of cells is an important indicator of normal cellular function. It is used as a parameter to study mitochondrial function as well as a marker of factors triggering the switch from healthy oxidative phosphorylation to aerobic glycolysis in cancer cells. Oxygen consumption is traditionally measured by a cumbersome oxygen electrode, a specialized piece of equipment that typically yields low sample throughput. The phosphorescent oxygen probe, MitoXpress®Xtra, developed by Luxcel Biosciences offers a novel method for analyzing oxygen consumption in whole cells. Cayman’s cell-based Oxygen Consumption Rate Assay Kit (MitoXpress® - Xtra HS Method) utilizes this newly developed phosphorescent oxygen probe to measure oxygen consumption rate in living cells. Antimycin A, an inhibitor of oxidation in the mitochondrial electron transport chain, is included to be used as a positive control. Glucose oxidase is also included in the kit to be used as a reference for oxygen depletion. The kit is easy to use and can be easily adapted to high throughput screening for compounds which modulate oxygen consumption rate.
600800
14.03.13
TP53BP1 tudor-like region (human recombinant)
Source: recombinant N-terminal GST-tagged protein expressed in E. coli · Mr: 42.6 kDa ·
14073
13.03.13
JMJD2A tudor domains (human recombinant)
Source: recombinant N-terminal GST-tagged protein expressed in E. coli · Mr: 42.2 kDa ·
14134
13.03.13
Memantine (hydrochloride)
An NMDA receptor antagonist
Memantine is an N-methyl-D-aspartate (NMDA) open-channel blocker (Ki = 1.2 μM at -60 mV) and uncompetitive antagonist with known anti-Parkinsonian, anti-epileptic, anti-stroke, and anti-Alzheimer’s disease properties. At 12 μM memantine blocks 90% of NMDA receptor activity and prevents NMDA-receptor mediated neurotoxicity resulting from excessive levels of glutamate in rat cortical and retinal ganglion cell neurons.
14184
12.03.13
Bilobalide
A neuroprotective natural product
Bilobalide is a sesquiterpene lactone which is found in extracts of G. biloba. It has been shown to protect against cerebral edema, decrease cortical infarct volume, and reduce cerebral ischemic damage. Bilobalide, at 10 μM, reduces the release of glycine and glutamate from hippocampal slices under ischemic conditions. It also activates the rat constitutive androstane receptor at 100 μM and increases the levels and activities of several cytochrome P450 isoforms in rat liver microsomes.
14272
12.03.13
MS-1020
A cell-permeable inhibitor of JAK3
MS-1020 is a cell-permeable inhibitor of janus kinase 3 (JAK3), strongly inhibiting constitutive autophosphorylation of JAK3 in L540 cells when used at 30-50 μM. It is without effect on other JAK isoforms and several other kinases, including Src, Lyn, Akt, EGFR, and ERK1/2. Through its effects on JAK3, MS-1020 blocks phosphorylation of downstream signal transduction and activators of transcription isoforms, reducing the expression of anti-apoptotic genes, leading to cell death.
14273
12.03.13
W-5 (hydrochloride)
A low-affinity calmodulin antagonist
W-5 is a chlorine-deficient analog of W-7, the potent calmodulin antagonist that binds to calmodulin and inhibits Ca2+/calmodulin-regulated enzyme activities (Ki = 11 μM). W-5 is less active than its calmodulin antagonist counterpart, inhibiting CHO-K1, MCF-7 breast cancer, and human myeloid progenitor cell proliferation with IC50 values greater than 100 μM. As a weaker antagonist for calmodulin, W-5 is suitable for use as a control compound for understanding the specificity of other calmodulin antagonists.
14271
11.03.13
Prostaglandin E2 Ethanolamide-d4
An internal standard for the quantification of PGE2-EA
Prostaglandin E2 ethanolamide (PGE2-EA)-d4 contains four deuterium atoms. It is intended for use as an internal standard for the quantification of PGE2-EA by GC- or LC-mass spectrometry.
9001412
08.03.13
Bosentan
An antagonist of endothelin receptors
Bosentan is an antagonist of the endothelin receptors type A (Ki = 6.5 nM) and type B (Ki = 340 nM).
11731
07.03.13
Sulfenylated Protein Cell-Based Detection Kit
For the detection of sulfenic acid-modified proteins in living cells
Reactive oxygen species (ROS) react with proteins, resulting in protein modification, such as protein sulfenylation through the reversible oxidation of cysteine residues. Redox-sensitive cysteine residues in proteins can function as sensors of ROS and serve as molecular switches, activating or deactivating proteins, following a change in oxidative state. However, the accumulation of proteins with irreversible cysteine oxidation is a hallmark of stress-induced cellular damage associated with diseases like cancer. Cayman’s Sulfenylated Protein Cell-Based Detection Kit employs the cell-permeable and chemoselective DAz-2 probe to detect sulfenic acid-modified proteins in living cells. It can be used to monitor intracellular sulfenylated protein levels in living cells to discriminate between normal and pathological conditions or to help identify new pathways regulated by sulfenic acid formation.
600320
06.03.13
StemRegenin 1 (hydrochloride)
Antagonizes hematopoietic stem cell differentiation
StemRegenin 1 (SR1) is a purine derivative that antagonizes aryl hydrocarbon receptor signaling with an IC50 value of 127 nM in CD34+ cells, which results in sustained expression of CD34. Human embryonic stem cells cultured with SR1 show a 50-fold increase in cells expressing CD34 (EC50 =120 nM) and a 17-fold increase in cells that retain the ability to engraft immunodeficient mice. This effect is quickly reversed with removal of SR1, which leads to rapid cell differentiation. SR1 (hydrochloride) has a formulation with greater solubility in aqueous buffers than standard SR1 (Item No. 10625).
14268
05.03.13
Coumestrol
A naturally-occurring phytoestrogen
Coumestrol is a phytoestrogen that occurs naturally in soybeans, spinach, and clover. It competitively (vs. 17 β-estradiol, Item No. 10006315) binds the estrogen receptors ERα (IC50 = 11 nM) and ERβ (IC50 = 2 nM) and can induce ER-dependent gene expression in isolated cells. Coumestrol is also a weak antagonist of pregnane X receptor (IC50 = 12 μM) as well as a potential inverse agonist of the constitutive androstane receptor (EC50 = 30 μM).
11730
05.03.13
GSK-J2 (sodium salt)
A negative control compound for GSK-J1
GSK-J2 is a pyridine regio-isomer of GSK-J1 which poorly inhibits JMJD3 (IC50 > 100 μM), making it an appropriate negative control for in vitro studies involving GSK-J1. For in vivo research, cell-permeable prodrug forms of GSK-J1 and GSK-J2 are available as GSK-J4 (Item No. 12073) and GSK-J5 (Item No. 12074), respectively. See <http://www.thesgc.org/scientists/chemical_probes/GSKJ1> for more information.
12056
04.03.13
PP1 (Src Inhibitor)
Potent, selective Src family tyrosine kinase inhibitor
PP1 is a potent, reversible, ATP-competitive, and selective inhibitor of the Src family of protein tyrosine kinases. It inhibits p56lck (IC50 = 5 nM), p59fynT (IC50 = 6 nM), Hck (IC50 = 20 nM), and Src (IC50 = 170 nM) without significantly affecting the activity of EGFR kinase (IC50 = 250 nM), JAK2 (IC50 = 50 µM), or ZAP-70 (IC50 = 0.6 µM). PP1 inhibits anti-CD3-induced tyrosine phosphorylation of human T cells with an IC50 value of 600 nM. It exhibits antitumor activity by antagonizing both proliferation and the inhibition of apoptosis mediated by a stem cell factor/mast cell growth factor in hematopoietic and small cell lung cancer cell lines. PP1 also blocks TGF-β-mediated cellular responses by directly inhibiting type I TGF-β receptors (IC50 = 50 nM) in a manner unrelated to Src signaling.
14244
04.03.13
Wogonin
A flavonoid with anti-inflammatory and antitumor activities
Wogonin is an O-methylated flavonoid isolated from the root of the traditional Chinese herb S. baicalensis with anti-inflammatory, anti-oxidant, and neuroprotective activities. At concentrations of 5-50 μM, wogonin inhibits inflammatory activation of cultured brain microglia by diminishing LPS-induced TNF-α, IL-1β, and nitric oxide production. Wogonin at 75 μM demonstrates tumor therapeutic potential inducing sub-G1 phase apoptosis through activation of caspase-3 activity in human osteocarcinoma cell lines.
14248
01.03.13
Naringenin
A citrus-derived flavonoid
Naringenin is a citrus-derived flavonoid that inhibits CYP3A4 activity in human liver microsomes (IC50s = 139-188 μM). At 100 mg/kg/day, naringenin selectively inhibits the transcription of Smad3 and directly down-regulates TGF-β1, significantly reducing lung metastasis in mice with bleomycin-induced pulmonary fibrosis. Naringenin demonstrates both lipid lowering and insulin-like properties in low-density lipoprotein (LDL) receptor-deficient mice fed a Western diet containing 1-3% naringenin by correcting VLDL overproduction, ameliorating hepatic steatosis, and attenuating dyslipidemia without affecting caloric intake or fat absorption.
14173
01.03.13
PX 12
An irreversible inhibitor of thioredoxin-1
PX 12 is a competitive, irreversible inhibitor of thioredoxin 1 (Trx1), acting by binding to Cys73 of this enzyme. As Trx1 is overexpressed in certain cancers, PX 12 is effective in suppressing the growth of cancer cells, with growth inhibition in a panel of 60 human tumors significantly correlated with expression of Trx1 mRNA. Through its effects on Trx1, PX 12 reduces hypoxia-induced HIF-1α protein levels (IC50 = 7.2 μM), as well as expression of VEGF (IC50 = 10.4 μM) and iNOS (IC50 = 18.1 μM), culminating in attenuation of the proliferation of MCF-7 cells (IC50 = 1.9 μM) and HT-29 cells (IC50 = 2.9 μM) as well as reduced microvessel density in MCF-7 tumor xenografts. PX 12 also blocks Trx-mediated activation of extracellular transglutaminase 2 (IC50 = ~3 μM) and Trx-1-increased expression and translation of CYP1B1.
14192
28.02.13
Crizotinib
A c-MET and ALK receptor tyrosine kinase inhibitor
Crizotinib is a derivative of aminopyridine that acts as a potent, orally bioavailable, ATP-competitive small-molecule dual inhibitor of c-MET (IC50 = 8 nM) and ALK (IC50 = 20 nM) receptor tyrosine kinases. Crizotinib shows antitumor efficacy, including cytoreductive antitumor activity, in multiple tumor models implanted in athymic mice that express activated c-MET or ALK fusion proteins (IC50s = 5-20 nM). Crizotinib is currently undergoing active clinical investigation in non-small cell lung cancer and phase I/II studies are being conducted in patients with anaplastic large cell lymphoma or neuroblastoma.
12087
28.02.13
Polymyxin B (sulfate)
A cationic peptide antibiotic
Polymyxin B (sulfate) is a mixture of at least four closely related components, polymyxin B1 to B4, with polymyxin B1 (Item No. 14074) and B2 being the two major components. Polymyxin B (sulfate) has rapid in vitro bactericidal activity against major multidrug-resistant Gram-negative bacteria, such as P. aeruginosa, A. baumannii, and K. pneumoniae.
14157
27.02.13
ITF 2357
HDAC inhibitor with anti-inflammatory and antineoplastic activities
ITF 2357 inhibits class I and class II histone deacetylases (maize HDACs: HD2, HD-1B, and HD-1A with IC50s = 7.5-16 nM) and reduces the production of several pro-inflammatory cytokines including TNFα, IL-1α, and IL-1β (IC50s = 10-22 nM). ITF 2357 also has activity against cells expressing janus kinase 2 (JAK2)V617F (IC50s = 1-10 nM), a mutated form of the JAK2 enzyme that is implicated in the pathophysiology of many myeloproliferative diseases, including polycythaemia vera.
11045
22.02.13
(±)-β-Hydroxybutyrate-d4 (sodium salt)
An internal standard for the quantification of (±)-β-hydroxybutyrate (sodium salt) by GC- or LC-MS
(±)-β-Hydroxybutyrate-d4 (sodium salt) contains four deuterium atoms at the 3, 4, 4, and 4 positions. It is intended for use as an internal standard for the quantification of (±)-β-hydroxybutyrate (sodium salt) by GC- or LC-mass spectrometry.
14158