New Products


New products at Cayman:


Intro Product Cat No Image
10.03.10
AdPLA2 Polyclonal Antibody
For immunochemical detection of AdPLA2
Antigen: human AdPLA2 amino acids 147-162 (MSLIGVMFSRNKRQKQ) · Host: rabbit · Application(s): WB ·
10337
10.03.10
PIK-75
A selective p110α inhibitor
PIK-75 is an imidazopyridine that selectively inhibits p110α with an IC50 value of 5.8 nM. It inhibits p110γ and p110β considerably less effectively with IC50 values of 0.076 µM and 1.3 µM, respectively. In adipocytes and myotubes, PIK-75 blocks production of PIP2 and/or PIP3, phosphorylation of Akt, and activation of mTORC1.
10009210
10.03.10
W146 (trifluoroacetate salt)
A selective S1P1 receptor antagonist
W146 is a S1P1 receptor antagonist that exhibits a Ki value of 77 nM for the human receptor in a GTP-γS binding assay with equipotency at the murine S1P1 receptor (2a = W146; 2b = W140 in supplemental material). No agonist or antagonist activity was observed at 10 µM W146 at S1P2, S1P3, or S1P5 receptors. W146 is active in vivo causing skin capillary leakage in murine lung and skin as well as inhibition of S1P1 agonist-induced lymphocyte sequestration. The half-life of W146 in rat blood is 73 minutes.
10009109
09.03.10
SC-51322
A selective EP1 antagonist
SC-51322 is a selective EP1 antagonist that inhibits PGE2 signaling in a guinea pig ileum muscle strip assay with a pA2 value of 8.1 and demonstrates analgesic activity in a murine writhing assay with an ED50 value of 0.9 mg/kg. It is pharmacologically similar to SC-51089, but does not release hydrazine, a known carcinogen to rats, as does SC-51089. SC-51322 potentiates the vasorelaxation of human pulmonary vein induced by PGE2 with an EC50 value of 7.75 µM.
10010744
09.03.10
SET8 Methyltransferase Inhibitor Screening Assay Kit
A convenient method for screening human SET8 inhibitors
Cayman’s SET8 Methyltransferase Inhibitor Screening Assay provides a convenient method for screening human SET8 inhibitors. The transfer of the methyl group from SAM by SET8 to the acceptor peptide (H4K20) generates S-adenosylhomocysteine, which is rapidly converted to S-ribosylhomocysteine and adenine by adenosylhomocysteine nucleosidase. This rapid conversion prevents the buildup of adenosylhomocysteine and its feedback inhibition on the methylation reaction. Finally, the adenine is converted to hypoxanthine by adenine deaminase, which in turn is converted to urate and hydrogen peroxide (H2O2). The reaction between H2O2 and 10-acetyl-3,7-dihydroxyphenoxazine (ADHP) produces the highly fluorescent compound resorufin. Resorufin fluorescence is analyzed using an excitation wavelength of 530-540 nm and an emission wavelength of 585-595 nm.
700350
09.03.10
SureLight® Western Kit (P112)
Save time and money with Columbia Bioscience’s Western blot detection kits. SureLight® Western kits provide the same sensitivity as enzymatic chemiluminescence (ECL) and enzymatic chemifluorescence (ECF) reagents. These assays are up to 16X more sensitive than other fluorescent kits. So, you can loose the enzyme and save up to an hour in processing your blots but keep the sensitivity. The Western Kit (P112) features sensitive fluorescent detection with a Goat Anti-Mouse SureLight® P3 conjugate. Sufficient buffers and detection reagent are provided for up to ten 10 x 10 cm2 blots.
13749
09.03.10
SureLight® Western Kit (P114)
Save time and money with Columbia Bioscience’s Western blot detection kits. SureLight® Western kits provide the same sensitivity as enzymatic chemiluminescence (ECL) and enzymatic chemifluorescence (ECF) reagents. These assays are up to 16X more sensitive than other fluorescent kits. So, you can loose the enzyme and save up to an hour in processing your blots but keep the sensitivity. The Western Kit (P114) features sensitive fluorescent detection with a Goat Anti-Rabbit SureLight® P3 conjugate. Sufficient buffers and detection reagent are provided for up to ten 10 x 10 cm2 blots.
13767
08.03.10
2-amino-4-phenyl Thiazole
A synthetic intermediate useful for pharmaceutical synthesis
2-amino-4-phenyl Thiazole is a synthetic intermediate useful for pharmaceutical synthesis.
13388
08.03.10
Donepezil
AChE inhibitor used to treat Alzheimer’s disease
Donepezil is a reversible acetylcholinesterase inhibitor that readily crosses the blood-brain barrier to reduce the breakdown of acetylcholine. As acetylcholine modulates plasticity, excitability, and arousal in the central nervous system, donepezil is commonly used in the treatment of Alzheimer’s disease to improve cognition, memory, and behavior. It has a half-life in circulation of about 70 hours. In this way, it is intended to prevent or reverse dementia. Studies on these effects have been equivocal, indicating that more research into the therapeutic potential of donepezil is warranted.
13245
08.03.10
Pristimerin
Potent, selective inhibitor of monoacylglycerol lipase
Pristimerin is a naturally occurring terpenoid that potently inhibits MAGL (IC50 = 93 nM). Its actions are rapid, reversible, and noncompetitive. Pristimerin (1 µM) significantly increases 2-AG levels in isolated rat neurons, indicating that it inhibits endogenous MAGL in cultured cells. Moreover, it does not increase levels of palmitoyl ethanolamide, suggesting that pristimerin does not affect the activity of fatty acid amide hydrolase (FAAH).
13621
08.03.10
SET7/9 (FL) Polyclonal Antibody
Antigen: human recombinant SET7/9 (amino acids 1-366) · Host: rabbit · Application(s): WB ·
13780
04.03.10
CYP3A4 Induction STEP™ Reporter Assay Kit (Luminescence)
A novel method to assess CYP3A4 induction
Cayman’s CYP3A4 Induction STEP™ Reporter Assay Kit (Luminescence) consists of a 96-well plate coated with a STEP™ complex containing a Secreted Alkaline Phosphatase (SEAP) reporter regulated by the human CYP3A4 gene promoter. The complex also contains two nuclear expression constructs, Pregnane X Receptor (PXR) and Hepatocyte Nuclear Factor-4α (HNF-4α). Cells grown on the CYP3A4 STEP™ Plate will introduce the reporter gene and express the PXR and HNF4 factors. Binding of inducer-activated transcription factors to the CYP3A4 promoter initiates a signal resulting in expression of SEAP, which is secreted into the cell culture medium. Aliquots of medium are removed at time intervals beginning at about 24 hours and SEAP activity is measured simply by adding a luminescence-based alkaline phosphatase substrate provided in the kit. The kit is simple to use and can be easily adapted to high-throughput screening for potential CYP3A4 inducers. A known CYYP3A4 inducer, rifampicin, is included in the kit for use as a positive control. The kit provides sufficient reagent to measure SEAP activity at three time points using the white plates provided.
600270
04.03.10
Palmitoyl Ethanolamide-d5
An internal standard for the quantification of PEA
An internal standard for the quantification of rosiglitazone by GC- or LC-MS
9000573
03.03.10
CD36 Monoclonal Antibody (Clone JC63.1) (azide free)
Antigen: recombinant adenovirus expressing full-length mouse CD36 · Host: CD36 null mouse (clone JC63.1) · Application(s): ICC, FC, and functional blocking ·
10009893
01.03.10
Corticosterone EIA Kit
A competitive assay for the quantification of corticosterone in plasma and fecal samples
Limit of detection: 80% B/B0: 30 pg/ml · Sensitivity: 50% B/B0: 150 pg/ml · Cayman’s Corticosterone EIA Kit is a competitive assay that can be used for quantification of corticosterone in plasma and fecal samples.
500655
01.03.10
HDAC4 (human recombinant)
Application(s): enzyme kinetics, inhibitor screening, and selectivity profiling · Source: N-terminal GST-tagged protein from baculovirus expression system · Mr: 75.2 kDa ·
10009652
25.02.10
H-1152 (hydrochloride)
Rho kinase inhibitor
H-1152 is a potent, specific, ATP-competitive, and cell permeable inhibitor of ROCK (Ki = 1.6 nM). It is a more potent inhibitor of ROCK than either Y-27632 (Ki = 140 nM) or HA-1077 (Ki = 330 nM). H-1152 poorly inhibits PKA, PKC, and myosin light chain kinase (Ki = 0.63, 9.27, and 10.1 μM, respectively). It has been used to examine the role of ROCK in such diverse processes as stress fiber assembly, vasoconstriction, as well as spontaneously tonic smooth muscle and neurite extension.
10007653
25.02.10
W140 (trifluoroacetate salt)
An inactive enantiomer of W146
W140 (trifluoroacetate salt) is an inactive enantiomer of W146, a selective S1P1 antagonist (Ki = 77 nM), that binds to the S1P1 receptor with a Ki of 4.6 µM (2a = W146; 2b = W140 in supplemental material). It exhibits no biological activity in vivo and can therefore serve as an effective control compound for experiments involving W146.
10009110
19.02.10
Aspalatone
An antithrombic compound
Aspalatone is an anti-platelet aggregator (IC50 = 180 µM, in vitro) that prolongs bleeding time significantly in a rodent model of thromboembolism. Additionally at a minimal effective dose of 24 mg/kg, aspalatone generates antioxidant and neuroprotective effects against kainic acid-induced epilepsy in rat hippocampus.
13644
19.02.10
Cystathionine γ-Lyase (human recombinant)
Source: Recombinant protein expressed in E. coli · Mr: 44.5 kDa ·
10329
19.02.10
Dimebolin (hydrochloride)
Neuroprotective drug
Dimebolin (hydrochloride), also known as Dimebon™, is an orally-available drug, approved in Russia for use as a non-selective antihistamine, that has shown promise in the treatment of neurodegenerative diseases, including Alzheimer’s disease and Huntington’s disease. In addition to preventing the onset and progression of disease by being neuroprotective, Dimebolin appears to promote clinical improvement by increasing cognitive function. At the cellular level, Dimebolin appears to have diverse effects, inhibiting the neurotoxic action of β-amyloid and blocking L-type calcium channels, inhibiting NMDA-type glutamate receptors, and preventing mitochondrial leakage. The hydrochloride form of Dimebolin is soluble in both aqueous and organic solvents.
10011349
19.02.10
NF-κB (p65) (Ser276) Inhibitory Peptide Set
A peptide inhibitor of NF-κB p65 phosphorylation
NF-κB has been shown to regulate the expression of a number of genes whose products are involved in inflammation, viral replication, carcinogenesis, antiapoptosis, invasion, and metastasis. Specific adhesion molecules, chemokines, inflammatory cytokines, and cell cycle regulatory genes are affected. Thus, agents that can suppress NF-κB activation have the potential to be treatments for inflammatory diseases and cancer. The Ser276 site of p65 is phosphorylated during NF-kB activation, allowing p65 nuclear translocation. This p65 inhibitory peptide contains a Ser276 site that is phosphorylated during NF-κB activation, thereby blocking p65 Ser276 phosphorylation. The NF-kB (p65) (Ser276) inhibitory peptide, also known as PTD-p65-P1, also contains a protein transduction (PTD) sequence (DRQIKIWFQNRRMKWKK) derived from antennapedia which renders the peptide cell permeable. The control peptide consists of only the PTD sequence.
13758
19.02.10
NF-κB (p65) (Ser529,536) Inhibitory Peptide Set
A peptide inhibitor of NF-κB p65 phosphorylation
NF-κB has been shown to regulate the expression of a number of genes whose products are involved in inflammation, viral replication, carcinogenesis, apoptosis, invasion, and metastasis. Specific adhesion molecules, chemokines, inflammatory cytokines, and cell cycle regulatory genes are affected. Thus, agents that can suppress NF-κB activation have the potential to be treatments for inflammatory diseases and cancer. The Ser529,536 sites of p65 are phosphorylated during NF-κB activation, allowing p65 nuclear translocation. This p65 inhibitory peptide contains the Ser529,536 sites that are phosphorylated during NF-κB activation, thereby blocking p65 phospho-Ser529,536 phosphorylation. The NF-κB (p65) (phospho-Ser529,536) inhibitor peptide can inhibit binding of recombinant p65 protein to DNA in a dose-dependent manner with maximum inhibition occuring at 50 µM. It can also inhibit TNF-induced NF-κB activation in cells. The NF-κB (p65) (Ser529,536) inhibitory peptide also contains a protein transduction (PTD) sequence (DRQIKIWFQNRRMKWKK) derived from antennapedia which renders the peptide cell permable. The control peptide consists of only the PTD sequence.
13759
18.02.10
Biotin-XX hydrazide
A biotinylating reagent
Biotin-XX hydrazide is a biotylating reagent for carbohydrates and carbonyl compounds that contains two aminohexanoic spacers to increase the efficiency of avidin-binding by alleviating steric hindrance.
13304
18.02.10
SIRT6 Direct Fluorescent Assay Kit
For fluorescent analysis of SIRT6
Cayman’s SIRT6 Direct Fluorescent Screening Assay provides a convenient fluorescence-based method for screening SIRT6 inhibitors or activators. The procedure requires only two easy steps, both performed in the same microplate. In the first step, the substrate, which comprises the p53 sequence Arg-His-Lys-Lys(ε-acetyl)-AMC, is incubated with human recombinant SIRT6 along with its cosubstrate NAD+. Deacetylation sensitizes the substrate such that treatment with the developer in the second step releases a fluorescent product. The fluorophore can be easily analyzed using an excitation wavelength of 350-360 nm and emission wavelength of 450-465 nm.
700290
17.02.10
trans-Zeatin
A plant growth regulator
trans-Zeatin is a member of the plant hormone family known as ‘cytokinins’, which regulate cell division, development, and nutrient processing. The biosynthesis of cytokinins involves isoprenylation of ATP or ADP, with trans-Zeatin being produced by the removal of phosphate and riboside groups from adenine and oxidation by cytochrome P735A. trans-Zeatin evokes its effects through high affinity receptors, including Arabidopsis histidine kinases (AHK). The affinity of trans-zeatin for AHK3, which is important in mediating plant development, has been reported to be 1.3 nM.
13226
16.02.10
CAY10621
Selective inhibitor of sphingosine kinase 1
CAY10261 is a selective inhibitor of SphK1, both in vitro (IC50 = 3.3 μM) and in U937 cells overexpressing human SphK1 (70 % inhibition at 5 μM). It has no inhibitory effect on SphK2 either in vitro or in cells. Similarly, CAY10261 does not reduce the activity of protein kinase C (PKC) except at very high concentration (>75 μM).
13371
16.02.10
Terbinafine (hydrochloride)
An antimycotic agent that inhibits squalene epoxidase
Terbinafine is an antifungal compound that is highly active against dermatophytes, mold, other basic fungi, and some strains of yeast. It is clinically used to treat nail and skin infections, inhibiting ergosterol synthesis at the stage of squalene epoxidation (IC50 = 30 nM for Candida albicans). At 90-120 µM, terbinafine exhibits antitumor and antiangiogenic activity by inducing cell cycle arrest at the G0/G1 stage in COLO 205 tumor cells and human vascular endothelial cells.
10011619
15.02.10
Griffithsin
Source: Recombinant N-terminal His-tagged GRFT, purified from E. coli · Mr: 14.6 kDa ·
10340
15.02.10
RSC-3388
cPLA2 inhibitor
RSC-3388 is a pyrrolidine derivative that acts as a potent inhibitor of cPLA2α, suppressing both recombinant human cPLA2 in vitro (IC50 = 1.8 nM) and cellular PLA2 activity in cells stimulated with the calcium ionophore A23187 (IC50 = 22 nM). In the human acute monocytic leukemia cell line THP-1, RSC-3388 blocks the production of prostaglandin E2 (IC50 = 31 nM) and leukotriene C4 (IC50 = 13 nM). RSC-3388 also reduces skin inflammation in mouse models of atopic dermatitis, presumably through its inhibitory effects on cPLA2.
13343
12.02.10
2-amino Pyridyl-5-thioamide
A synthetic intermediate useful for pharmaceutical synthesis
2-amino Pyridyl-5-thioamide is a synthetic intermediate useful for pharmaceutical synthesis.
13389
12.02.10
Anacardic Acid
A histone acetyltransferase inhibitor
Anacardic acid, isolated from cashew shells or several other medicinal plants, is the general name given to a family of four different 6-alkyl salicyclic acids having varying degrees of unsaturation in the 15-carbon alkyl chain. These compounds are associated with anti-inflammatory, anti-tumor, molluscicidal, and anti-microbial activity. Literature frequently sites and gives the name anacardic acid to the completely-saturated compound (6-pentadecyl salicylic acid). Anacardic acid inhibits the histone acetyltransferase (HAT) activity of the transcription co-activators p300 and p300/CREB-binding protein-associated factor (pCAF) with IC50 values of 8.5 and 5 µM, respectively. At 25 µmol/L, anacardic acid suppresses NF-κB activation, inhibits IκB-α phosphorylation, and prohibits p65 nuclear translocation in KBM-5 cells.
13144
12.02.10
Arachidonic Acid methyl ester-d8
An internal standard for quantification of arachidonic acid methyl ester by GC- or LC-MS
390014
11.02.10
Atrazine
An herbicide
Atrazine is an herbicide that is effective in controlling a broad range of weeds. Atrazine has been reported to cause cancer in certain laboratory animals, have diverse effects on the reproductive system in animals and humans, and disrupt the normal function of the endocrine system. Chronic exposure of frogs to atrazine significantly alters the expression of several genes, especially those involved in growth and metabolism. The United States Environmental Protection Agency currently allows the use of atrazine as an herbicide but, in 2009, launched a comprehensive new evaluation to determine its effects on humans.
13375
11.02.10
Icariin
A PDE5 inhibitor
Icariin, the active component of the Chinese medicinal plant E. brevicornum, is an inhibitor of human recombinant PDE5 with an IC50 value of 5.9 µM. It is a prenylated flavonol that has been used to treat erectile dysfunction and has been shown to have anti-cancer and antioxidant activity. At a concentration of 1 x 107 mol/L, icariin induces differentiation of cardiomyocytes and upregulates the expression of cardiac genes. At 20 µg/ml, icariin increases the proliferation and differentiation of cultured human osteoblasts, which appears to be mediated in part by upregulating bone morphogenetic protein 2 mRNA.
13624
11.02.10
Iressa
An EGFR inhibitor
Iressa is a selective EGFR-TK inhibitor that blocks the growth of GEO colon cancer, ZR-75-1 and MCF-10A Ha-ras breast cancer, and OVCAR-3 ovarian cancer cell lines with IC50s ranging between 0.2 - 0.4 µM. By interfering with the intracellular kinase domain, iressa prevents EGFR autophosphorylation and prevents downstream signal transduction. Iressa has been used to treat advanced (or recurrent) non-small cell lung cancer (NSCLC). However, the FDA retracted its general approval for this compound when a phase III trial failed to demonstrate an overall survival benefit. Iressa appears to be most efficacious in treating certain EGFR gene mutations that are prevalent in Asian populations.
13166
11.02.10
N-Benzylacetamidine (hydrobromide)
Potent, selective inhibitor of iNOS
N-Benzylacetamidine is a potent inhibitor of iNOS (IC50 = 0.20 μM), with over 1,000-fold selectivity compared to eNOS (IC50 = 350 µM).
13570
11.02.10
NF-κB (p65) Monoclonal Antibody-biotin (Clone 112A1021)
For immunochemical analysis of NF-κB (p65)
Antigen: synthetic peptide corresponding to human NF-κB (p65) amino acids 526-539 · Clone designation: 112A1021 · Host: mouse · Isotype: IgG1κ · Application(s): ELISA ·
13756
11.02.10
NF-κB (p65) Monoclonal Antibody (Clone 112A1021)
For immunochemical analysis of NF-κB (p65-NLS)
Antigen: synthetic peptide corresponding to human NF-κB (p65) amino acids 526-539 · Clone designation: 112A1021 · Host: mouse · Isotype: IgG1κ · Application(s): FC, IHC, and WB ·
13752
11.02.10
NF-κB (p65) NLS Polyclonal Antibody
For immunochemical analysis of NF-κB (p65-NLS)
Antigen: a portion of the NF-κB (p65) NLS · Host: rabbit · Application(s): ICC and WB ·
13751
11.02.10
NF-κB (p65) Polyclonal Antibody (aa 2-17)
For immunochemical analysis of NF-κB (p65)
Antigen: synthetic peptide corresponding to human NF-κB (p65) amino acids 2-17 · Host: rabbit · Application(s): WB ·
13757
11.02.10
NF-κB (p65) Polyclonal Antibody (aa 538-546)
For immunochemical analysis of NF-κB (p65)
Antigen: synthetic peptide corresponding to human NF-κB (p65) amino acids 538-546 · Host: rabbit · Application(s): WB ·
13753
10.02.10
JZL 195
Dual FAAH and MAGL inhibitor
JZL 195 is a potent inhibitor of both FAAH and MAGL (IC50 = 2 and 4 nM, respectively). It poorly inhibits neuropathy target esterase and ABHD6 and does not inhibit other brain serine hydrolases. JZL 195 displays time-dependent inhibition of FAAH and MAGL in vivo, consistent with a covalent mechanism of activation. The in vivo inhibitory actions of JZL 195 against FAAH and MAGL are comparable to those of the selective inhibitors PF-3845 (Catalog No. 13279) and JZL 184 (Catalog No.13158), respectively. Through its inhibitory actions, JZL 195 simultaneously augments brain levels of AEA and 2-AG, producing antinociceptive, cataleptic, and hypomotility effects like those produced by direct CB1 agonists.
13668
10.02.10
NF-κB (p50) NLS Inhibitory Peptide Set
A tool for studying nuclear translocation of NF-κB
The nuclear localization signal (NLS) sequence is required for nuclear translocation of NF-κB (p50). In un-stimulated cells, NF-κB is in the cytoplasm in an inactive form and the NLS is masked. The degradation of IkBa during NF-κB signaling unmasks the NLS of NF-κB subunits and NF-κB is translocated to the nucleus. The p50 inhibitory peptide contains the (p50) NLS sequence (VQRKRQKLM) and blocks the intracellular recognition mechanism for the NLS present on p50. Consequently p50 nuclear translocation is blocked. The (p50) NLS inhibitory peptide also contains a protein transduction (PTD) sequence (DRQIKIWFQNRRMKWKK) derived from antennapedia which renders the peptide cell permeable. The control peptide consists of only the PTD sequence.
13760
09.02.10
Sphingomyelinase Inhibitor Screening Assay Kit
A convenient method for screening sphingomyelinase inhibitors
Cayman’s Sphingomyelinase Inhibitor Screening Assay provides a convenient method for screening sphingomyelinase inhibitors. This assay includes a neutral bacterial SMase. Even though bacterial SMase only shares a 20% sequence homology with mammalian neutral SMase, it has been shown to share a common catalytic site as the mammalian SMase and similar inhibition profile. Cleavage of the sphingomyelin conjugate by SMase results in the release of a ceramide analog containing a free thiol which is detected by the fluorescent SMase Detector. This fluorescence is analyzed with an excitation wavelength of 375-385 nm and an emission wavelength of 510-520 nm.
700330
05.02.10
MyD88 Homodimerization Inhibitory Peptide Set
A peptide inhibitor of MyD88 dimerization
MyD88 is an adapter protein that links toll-like receptors (TLRs) and interleukin-1 receptors (IL-1Rs) with downstream signaling molecules. Homodimerization of MyD88 is a critical step in the signaling process and allows the recruitment and activation of the kinase IRAK. MyD88 exists as a homodimer when recruited to activate TLR/IL-receptors (TIR). The inhibitor peptide contains a sequence from the MyD88 TIR homodimerization domain. MyD88 monomer binds to this inhibitor peptide, thereby blocking Myd88 homodimerization. The MyD88 homodimerization inhibitory peptide contains a protein transduction (PTD) sequence (DRQIKIWFQNRRMKWKK) derived from antennapedia which renders the peptide cell permeable. The control peptide consists of only the PTD sequence.
13748
05.02.10
MyD88 Polyclonal Antibody
For immunochemical analysis of MyD88
Antigen: synthetic peptide corresponding to human MyD88 amino acids 233-248 · Host: rabbit · Application(s): WB ·
13746
05.02.10
NF-κB (p50) Monoclonal Antibody (Clone 2J10D7)
For immunochemical analysis of NF-κB (p50)
Antigen: a portion of amino acids 150-200 of human NF-κB (p50) · Clone designation: 2J10D7 · Isotype: IgG1κ · Application(s): IHC and WB ·
13755
05.02.10
Oxalomalic Acid (sodium salt)
An aconitase inhibitor
Oxalomalic acid, formed by the condensation of oxaloacetate with glyoxylate in vivo, inhibits both aconitase and NADP-dependent isocitrate dehydrogenase in the conversion of citrate to isocitrate at concentrations as low as 1 mM. At 5 mM, oxalomalic acid inhibition of aconitase leads to a decrease in the binding activity of IRP1 and a decrease in glutamate secretion in cultured lens epithelial cells, retinal pigment epithelial cells, and neurons.
13521
05.02.10
YK-4-279
An inhibitor of Ewing’s sarcoma tumors
YK-4-279 is an inhibitor of protein-protein interactions between ES-FLI1 and RHA. At 10 µM, YK-4-279 blocks RHA binding to ES-FLI1 and induces apoptosis of a panel of Ewing’s sarcoma tumor cell lines with IC50 values ranging from 0.5 to 2 µM. At 1.5 mg per dose, YK-4-279 reduces the growth of Ewing’s sarcoma orthotopic xenografts in mice after treatment with the inhibitor for two weeks.
13661
03.02.10
L-DOPA
A dopamine precursor used to treat Parkinson’s Disease
L-DOPA is a metabolic precursor of dopamine that is capable of crossing the blood brain barrier. It is produced from L-tyrosine by trysosine hydroxylase and metabolized by catechol-O-methyl transferase (COMT). In the brain L-DOPA is converted to dopamine. It is conventionally used to increase dopamine concentrations in the brain as a treatment for Parkinson’s disease and stroke recovery. However L-DOPA has a short half-life and is known to elevate homocysteine concentrations in plasma, which can be neurotoxic and induce oxidative damage.
13248
02.02.10
13,14-dihydro-16,16-difluoro Prostaglandin J2
Analog of PGJ2
13,14-dihydro-16,16-difluoro PGJ2 is an analog of PGJ2. While its biological activities have not been evaluated, it should be noted that the addition of two electron-withdrawing fluorine atoms has been used to stabilize prostanoids and significantly delay degradation in vivo. Importantly, 13,14-dihydro PGE1 has activity that is comparable to that of PGE1, suggesting that this analog of PGJ2 could be biologically active.
13635
02.02.10
SC-51089
Selective EP1 antagonist
SC-51089 is a selective EP1 antagonist, first shown to have in vivo analgesic activity in mice (ED50 = 6.3 mg/kg when given subcutaneously) and in the rat. SC-51089 also inhibits the growth of glioma cell lines in vitro (IC50 = ~1 μM) and slows tumor growth in vivo. In addition, SC-51089 is neuroprotective, attenuating neuronal cell death in response to oxidative stress, an effect that is also found in EP1-/- mice and mediated by PGE2.
10011561
02.02.10
SU 11652
A potent RTK inhibitor
SU 11652 is a potent, cell-permeable, and ATP-competitive inhibitor of the tyrosine kinase activity of several GFRs, including platelet-derived GFR (PDGFR-β; IC50 = 3 nM), vascular endothelial GFR (VEGFR-2; IC50 = 27 nM), and fibroblast GFR (FGFR1; IC50 = 170 nM), but not epidermal GFR (EGFR; IC50 > 20 μM). SU 11652 also potently inhibits wild-type Kit in mast cells (IC50 = 50 nM) and stops cell cycling while inducing apoptosis in cells expressing constitutively-active Kit mutants. Furthermore SU 11652 reduces angiogenesis induced by estrogen in mice.
13577
29.01.10
Fucoxanthin
A carotenoid with anti-obesity actions
Fucoxanthin is a carotenoid that occurs naturally in certain algae. It significantly reduces abdominal white adipose tissue (WAT) in mice and rats when included in their diet. Fucoxanthin increases the amount of mitochondrial uncoupling protein 1 (UCP1), a fatty acid-stimulated protein involved in respiration and thermogenesis in WAT of mice and rats. In KK-Ay mice, which are used to model obese type 2 diabetics with hyperinsulinemia, fucoxanthin reduces WAT gain and also decreases blood glucose and plasma insulin levels.
13068
27.01.10
13,14-dihydro-16,16-difluoro Prostaglandin D2
Analog of PGD2
13,14-dihydro-16,16-difluoro PGD2 is an analog of PGD2. While its biological activities have not been evaluated, it should be noted that the addition of two electron-withdrawing fluorine atoms has been used to stabilize prostanoids and significantly delay degradation in vivo. Importantly, 13,14-dihydro PGE1 has activity that is comparable to that of PGE1, suggesting that this analog of PGD2 could be biologically active.
13612
27.01.10
13,14-dihydro-16,16-difluoro Prostaglandin F2α
Analog of PGF2α
13,14-dihydro-16,16-difluoro PGF2α is an analog of PGF2α. While its biological activities have not been evaluated, it should be noted that the addition of two electron-withdrawing fluorine atoms has been used to stabilize prostanoids and significantly delay degradation in vivo. Importantly, 13,14-dihydro PGE1 has activity that is comparable to that of PGE1, suggesting that this analog of PGF2α could be biologically active.
13609
27.01.10
Glycyl-H-1152 (hydrochloride)
Potent, selective inhibitor of Rho kinase II (ROCK-II)
Rho Kinase Inhibitor IV is a selective and potent Rho kinase inhibitor (IC50 = 11.8 nM for ROCK-II). It is a glycylated isoquinoline compound derived from the therapeutically-important ROCK inhibitor HA-1077 (Fasudil hydrochloride) and exhibits better specificity. Thus, it poorly inhibits calcium/calmodulin kinase II, protein kinase G, and Aurora A (IC50 = 2.57, 2.35, and 3.26 μM, respectively) as well as PKA or PKC (IC50 > 10 μM for each). The potency of Glycyl-H-1152 is superior to that of other ROCK inhibitors, including Y-27632 (Ki = 220 nM) and HA-1077 (IC50 = 158 nM).
13332
27.01.10
PF-3845
Inhibitor of FAAH
PF-3845 is a potent, selective, and irreversible inhibitor of FAAH (Ki = 0.23 μM). It covalently binds FAAH on Ser241 at the catalytic site, resulting in prolonged elevation of AEA in the brain and plasma in rats after treatment. PF-3845 significantly and persistently reduces inflammatory pain in rats through a cannabinoid receptor-dependent mechanism.
13279
25.01.10
AS 041164
Selective inhibitor of PI3Kγ
AS 041164 is a potent inhibitor of PI3K with selectivity for the class IB isoform PI3Kγ (IC50 = 70 nM), compared to PI3Kα (IC50 = 240 nM), PI3Kβ (IC50 = 1.45 μM), and PI3Kδ (IC50 =1.70 ). When tested at 1.0 μM, it shows little or no activity against 38 other common kinases. When given orally to mice, AS 041164 shows a pharmacokinetic profile that is similar to the general PI3K inhibitor LY294002 but is three times more potent (ED50 = 27.4 mg/kg for AS 041164 versus 81.6 mg/kg for LY294002) in blocking neutrophil recruitment induced by RANTES.
13622
25.01.10
Celastramycin A
An antibacterial and immunosuppressant
Celastramycin A is a bioactive compound isolated from endophytic bacteria living in plants of the Celastraceae family. This benzoyl pyrrole inhibits the growth of bacteria and mycobacteria, with a minimal inhibitory concentration as low as 0.05 μg/ml. Celastramycin A also suppresses the production of IL-8 in human umbilical vein endothelial cells as stimulated by TNF-α (IC50 = 0.01 μg/ml).
13519
25.01.10
Chemokine-Like Receptor 1 Polyclonal Antibody
Antigen: human CMKLR1 amino acids 358–371 (NERTSMNERETGML) · Host: rabbit · Application(s): WB, FC, and IHC ·
10325
21.01.10
Tamoxifen
Estrogen receptor modulator
Tamoxifen is a selective estrogen receptor modulator, evoking tissue-dependent effects. It is an antagonist of ER action in breast tissue and breast cancer cells and is reported to be effective in the treatment of early breast cancer to prevent tumor growth. Importantly, tamoxifen has been reported to act as an ER agonist in bone and blood vessels, helping to minimize osteoporosis and reduce the risk of cardiovascular disease in post-menopausal women. Also, tamoxifen is a partial ER agonist in uterine tissues and is reported to increase the risk of endometrial carcinoma.
13258
20.01.10
Palmitoyl Ethanolamide-d4
An internal standard for the quantification of PEA
9000551
19.01.10
ACS 67
An H2S-releasing latanoprost analog
ACS 67 is an analog of latanoprost (free acid) that contains a hydrogen sulfide releasing component conjugated to the latanoprost carboxyl group. In glaucomatous pigmented rabbits, ACS 67 reduced intra-ocular pressure (IOP) more rapidly and to a greater extent than latanoprost (15 versus 25.5 mm Hg at 4 hours) at a dose of 0.005% for each compound. ACS 67 also increased the levels of reduced glutathione and cGMP in the aqueous humor of glaucomatous pigmented rabbits better than latanoprost.
13619
19.01.10
Akt3 Monoclonal Antibody (Clone 66C1247.1)
For immunochemical analysis of Akt3
Antigen: synthetic peptide from human Akt3 amino acids 119-136 (CSPTSQIDNIGEEEMDAS); this sequence is identical in human, mouse, rat, sheep, dog, and chicken · Clone designation: 66C1247.1 · Host: mouse · Isotype: IgG1 · Application(s): WB ·
13736
19.01.10
GPR17 (C-Term) Polyclonal Antibody
Antigen: human GPR17 amino acids 351-367 (SFEGKTNESSLSAKSEL) · Host: rabbit · Peptide sequence: WB, FC, and ICC ·
10136
19.01.10
GPR55 Polyclonal Antibody
Antigen: human GPR55 amino acids 207-219 (ILLGRRDHTQDWV) · Host: rabbit · Application(s): WB, FC, and ICC ·
10224
18.01.10
Akt3 Polyclonal Antibody
For immunochemical analysis of Akt3
Antigen: synthetic peptide from human Akt3 amino acids 119-136; this sequence is identical in human, mouse, and rat · Host: rabbit · Application(s): WB ·
13737
18.01.10
Akt (Isoforms 1, 2, 3) Inhibitory Peptide Set
Peptide to block Akt1, Akt2, and Akt3 kinase activity
Akt is a protein kinase that plays a central role in inhibiting apoptosis through promoting cell survival. Activated Akt functions by phosphorylating downstream targets in survival signaling pathways. TCL1 (a proto-oncogene underlying human T-cell prolymphocytic leukemia) interacts with Akt through an N-terminal pleckstrin homology (PH) domain and functions as an Akt kinase co-activator. This inhibitory peptide interacts with Akt. The peptide binds to the PH domain of Akt and inhibits Akt1, Akt2, and Akt3 kinase activity. The Akt (Isoforms 1, 2, 3) inhibitory peptide also contains a protein transduction (PTD) sequence (DRQIKIWFQNRRMKWKK) derived from antennapedia which renders the peptide cell permeable. The control peptide consists of only the PTD sequence.
13738
18.01.10
FoxP3/Scurfin Polyclonal Antibody
For immunochemical analysis of FoxP3/Scurfin
Antigen: synthetic peptide corresponding to the exon 2 deletion site was used as immunogen · Host: rabbit · Application(s): IHC and WB ·
13739
18.01.10
FoxP3Δ2 (exon 2 deleted) Specific Monoclonal Antibody (Clone 16J4G6)
For immunochemical analysis of FoxP3Δ2
Antigen: synthetic peptide corresponding to the exon 2 deletion site · Clone designation: 16J4G6 · Host: Mouse · Isotype: IgMκ · Application(s): WB ·
13744
18.01.10
FoxP3Δ2 (exon 2 deleted) Specific Monoclonal Antibody (Clone 16J4G6) (azide free)
For immunochemical analysis of FoxP3Δ2
Antigen: synthetic peptide corresponding to the exon 2 deletion sit · Clone designation: 16J4G6 · Host: mouse · Isotype: IgMκ · Application(s): WB ·
13743
15.01.10
CFSE Cell Division Assay Kit
A flow cytometric assay to assess cell proliferation
Cayman’s CFSE Cell Division Assay Kit provides an easy to use format for labeling and tracing cells through successive cell divisions which can be used to study the induction and inhibition of cell division in any in vitro model. The kit contains sufficient reagents for labeling and analyzing 100 cell samples by flow cytometry. CFSE can also be combined with any fluorochrome compatible with fluorescein for use in flow cytometry.
10009853
13.01.10
Linoleoyl Ethanolamide-d4
An internal standard for the quantification of linoleoyl ethanolamide by GC- or LC-MS
9000553
12.01.10
Akt2/3 Polyclonal Antibody
For immunochemical analysis of Akt2/3
Antigen: synthetic peptide from human Akt2 amino acids 319-331; this sequence is 100% homologus in Akt3 · Host: rabbit ·
13735
12.01.10
Akt2 Monoclonal Antibody (Clone 95C567.1.2)
For immunochemical analysis of Akt2
Antigen: synthetic peptide from human Akt2 amino acids 106-123 · Clone designation: 95C567.1.2 · Host: mouse · Isotype: IgM · Application(s): WB ·
13734
12.01.10
Dimebolin
Neruroprotective drug
Dimebolin is an orally-available drug, approved in Russia for use as a non-selective antihistamine, that has shown promise in the treatment of neurodegenerative diseases, including Alzheimer’s and Huntington’s disease. In addition to reported activity in preventing the onset and progression of disease by being neuroprotective, dimebolin appears to promote clinical improvement by increasing cognitive function. At the cellular level, dimebolin appears to have diverse effects, inhibiting the neurotoxic action of β-amyloid and blocking L-type calcium channels, inhibiting NMDA-type glutamate receptors, and preventing mitochondrial leakage.
9000556
12.01.10
Oleoyl Ethanolamide-d4
An internal standard for the quantification of OEA by GC- or LC-MS
9000552
11.01.10
Akt1 (Phospho-Ser473) Monoclonal Antibody (Clone 104A282)
For immunochemical analysis of Akt1 (Phospho-Ser473)
Antigen: synthetic peptide from human Akt1 containing phospho-serine473 · Clone designation: 104A282 · Host: mouse · Isotype: IgG2κ · Application(s): IP and WB ·
13733
11.01.10
Akt1 Polyclonal Antibody
For immunochemical analysis of Akt1
Antigen: synthetic peptide from human Akt1 amino acids 464-477; this peptide sequence is identical in human, murine, chicken, and frog · Host: rabbit · Application(s): WB ·
13732
07.01.10
SET8 (human recombinant)
Source: recombinant N-terminal Histidine-tagged SET8 amino acids 190-352, purified from E. coli, NP-065115 · Mr: 21.1 kDa ·
10319
06.01.10
Alanine Transaminase Activity Assay Kit
A convenient method of detecting ALT activity in serum, plasma, tissue samples, and cell lysates
Cayman’s Alanine Transaminase Assay Kit provides a convenient method of detecting ALT activity in serum, plasma, tissue samples, and cell lysates. Measurement of the ALT activity is carried out by monitoring the rate of NADH oxidation in a coupled reaction system employing lactate dehydrogenase (LDH). The oxidation of NADH to NAD+ is accompanied by a decrease in absorbance at 340 nm. Under circumstances in which the ALT activity is rate limiting, the rate decrease is directly proportional to the ALT activity in the sample.
700260
06.01.10
Piroxicam
Non-selective NSAID
Piroxicam is a non-steroidal anti-inflammatory drug (NSAID) that non-selectively and reversibly inhibits both isoforms of cyclooxygenase (COX; IC50 = 1.57 and 1.69 μM for COX-1 and COX-2, respectively). It has an extended half-life of about 40 hours, which allows once daily administration leading to sustained plasma and tissue levels. In addition to its anti-inflammatory effects, piroxicam is known to be an effective analgesic that has been used extensively in the treatment of arthritis. It has also been used to inhibit COX activity for treatment of certain cancers in animals. As with other NSAIDs, the extended use of piroxicam results in damage to the gastrointestinal lining.
13368
06.01.10
SIRT4 (human recombinant)
Source: Recombinant N-terminal GST-tagged SIRT4 purified from E. coli · Mr: 61.9 kDa ·
10317
05.01.10
Melanocortin-3 Receptor STEP™ Reporter Assay Kit (Luminescence)
A cell-based screening assay based on novel transfection (STEP™) technology
Cayman’s Melanocortin 3 Receptor STEP™ Reporter Assay Kit (Luminescence) consists of a 96-well plate coated with both MC3R and Secretory Alkaline Phosphatase (SEAP) reporter constructs (MC3R STEP™ Plate). Cells grown on the STEP™ complex will express MC3R at the cell surface. Binding of agonists to MC3R initiates a signal transduction cascade resulting in expression of SEAP which is secreted into the cell culture media. Aliquots of media are removed at timed intervals, beginning at approximately six hours, and SEAP activity is measured following addition of a luminescence-based alkaline phosphatases substrate provided in the kit. The kit is simple to use and can be easily adapted to high throughput screening for therapeutic compounds regulating the activation of MC3R. A MC3R agonist, α-MSH (α-melanocyte-stimulating hormone), is included in the kit for use as a positive control. The kit provides sufficient reagent to measure SEAP activity at three time points, using the black plates included.
600180
05.01.10
Melanocortin-4 Receptor STEP™ Reporter Assay Kit (Luminescence)
A cell-based screening assay based on novel transfection (STEP™) technology
Cayman’s Melanocortin 4 Receptor STEP™ Reporter Assay Kit (Luminescence) consists of a 96-well plate coated with both MC4R and Secretory Alkaline Phosphatase (SEAP) reporter constructs (MC4R STEP™ Plate). Cells grown on the STEP™ complex will express MC4R at the cell surface. Binding of agonists to MC4R initiates a signal transduction cascade resulting in expression of SEAP which is secreted into the cell culture media. Aliquots of media are removed at timed intervals, beginning at approximately six hours, and SEAP activity is measured following addition of a luminescence-based alkaline phosphatases substrate provided in the kit. The kit is simple to use and can be easily adapted to high throughput screening for therapeutic compounds regulating the activation of MC4R. A MC4R agonist, α-MSH (α-melanocyte-stimulating hormone), is included in the kit for use as a positive control. The kit provides sufficient reagent to measure SEAP activity at three time points, using the black plates included.
600190
22.12.09
SIRT7 (human recombinant)
Source: Full length (2-400 aa) recombinant N-terminal hexahistidine tagged SIRT7, expressed in E. coli · Mr: 49.3 kDa ·
10316
22.12.09
trans-EKODE-(E)-Ib
Biologically active oxidative derivative of linoleic acid
trans-EKODE-(E)-Ib is a biologically active peroxidation product of linoleic acid that is characterized, structurally, by having a trans carbon-carbon double bond between the 9-keto and 12,13-epoxy groups. It activates an antioxidant response element (ARE) in neuronal cells and induces the expression of ARE-regulated cytoprotective genes like NQO1. This EKODE also stimulates the synthesis of aldosterone and corticosterone in adrenal cells when supplied at 1-5 μM. This effect appears to be mediated by a rise in intracellular calcium.
10004224
17.12.09
Methionine Sulfoxide Immunoblotting Kit
For the immunochemical detection of proteins containing MetO residues by western blotting
Cayman’s Methionine Sulfoxide (MetO) Immunoblotting Kit contains reagents needed for the immunochemical detection of proteins containing MetO residues by western blotting. MetO-containing samples of interest include those from cell or tissue lysates as well as semi-pure or purified proteins. Samples may be prepared with reducing or non-reducing sample buffer prior to SDS-PAGE and tested along side one SDS-PAGE well designated for the provided positive control. The MetO Polyclonal Antibody was isolated from rabbit serum generated after immunization with a oxidized corn protein (MetO-DZS18) rich in methionine. This polyclonal antibody is specific for protein methionine sulfoxide.
600160
10.12.09
Aldehyde Site (DNA and Protein) Detection Kit
For detection of aldehyde sites in cells
Cayman’s Aldehyde Site (DNA and Protein) Detection Kit employs an aldehyde reactive probe (ARP), O-(biotinylcarbazoylmethyl) hydroxylamine, as a probe to detect aldehyde sites in cells. Epigallocatechin Gallate (EGCG), a compound known to react with culture medium to generate hydrogen peroxide (H2O2) and cause DNA damage, is included to be used as a positive control. The kit is easy to use and can be easily adapted to high throughput screening for compounds imposing oxidative stress on cells or organisms.
600170
10.12.09
SIRT2 Direct Fluorescence Screening Assay Kit
A convenient fluorescence-based method for screening SIRT2 inhibitors or activators
Cayman’s SIRT2 Direct Fluorescent Screening Assay provides a convenient fluorescence-based method for screening SIRT2 inhibitors or activators. The procedure requires only two easy steps, both performed in the same microplate. In the first step, the substrate, which comprises the p53 sequence Gln-Pro-Lys-Lys(ε-acetyl)-AMC, is incubated with human recombinant SIRT2 along with its cosubstrate NAD+. Deacetylation sensitizes the substrate such that treatment with the Developer in the second step releases a fluorescent product. The fluorophore can be analyzed with an excitation wavelength of 350-360 nm and an emission wavelength of 450-465 nm.
700280
07.12.09
15(R)-Bimatoprost
Isomer of bimatoprost
15(R)-Bimatoprost is an isomer of bimatoprost, characterized by an inverted (β) hydroxyl group at C-15. While this isomer has not been characterized, the comparable inversion of 15-hydroxyl groups, from (S) to (R), on other PGF2α analogs typically decreases, but does not eliminate, activity.
10008127
07.12.09
Allopurinol
Inhibitor of xanthine oxidase
Allopurinol is an isomer of hypoxanthine that inhibits xanthine oxidoreductase (IC50 values between 0.2 and 50 μM, depending on assay and cell type). In vivo, allopurinol has been reported to effectively and safely lower serum and urinary uric acid levels and is also reported to be effective in the treatment of gout and hyperuricemia. Allopurinol is rapidly metabolized in vivo to the xanthine analog oxypurinol; which is a metabolite that clearly augments the therapeutic effect of allopurinol.
10012597
04.12.09
7(Z),11(Z)-Pentacosadiene
Sex pheromone in Drosophila
7(Z),11(Z)-Pentacosadiene is a 25-C hydrocarbon that is found in low abundance on cuticles of mature Drosophila females. Depletion of a female-specific elongase (eloF), which leads to an increase in 7(Z),11(Z)-pentacosadiene along with a parallel decrease in 7,11-nonacosadiene, significantly reduces copulation in Drosophila. This raises the possibility that 7(Z),11(Z)-pentacosadiene may act as an anti-aphrodisiac.
9000531
04.12.09
Acetyl Lysine Polyclonal Antibody-biotin
For immunochemical detection of acetylated lysine
Antigen: acetylated KLH · Host: rabbit · Application(s): WB, IP, ELISA, and IF ·
13725
04.12.09
Acetyl Lysine Polyclonal Antibody HRP Conjugate
For immunochemical detection of acetylated lysine
Antigen: acetylated KLH · Host: rabbit · Application(s): WB, IP, ELISA, and IF ·
13726
04.12.09
CAY10606
Inhibitor of 5-lipoxygenase
CAY10606 is a potent, reversible inhibitor of 5-LO, both in cell-free assays (IC50 = 86 nM) and in intact neutrophils (IC50 = 230 nM). It prevents the production of LTs in whole blood, whether 5-LO is activated with the calcium ionophore A23187 (IC50 = 1.6 μM) or formyl peptide (fMLP) following priming with lipopolysaccharide (IC50 = 830 nM). In rats subjected to carrageenan-induced pleurisy, CAY10606 significantly reduces both LT biosynthesis and the inflammatory reaction.
13381
04.12.09
Fatty Acid Screening Library (96-well)
For screening of variety of fatty acids
This screening plate contains a variety of fatty acids with diverse biological activities.
10504
04.12.09
Kir2.3 Potassium Channel Monoclonal Antibody (Clone S25-35)
For immunochemical detection of Kir2.3
Antigen: fusion protein amino acids 390-445 of human Kir2.3 · Clone designation: S25-35 · Host: Mouse · Isotype: IgG1 · Application(s): WB and IHC ·
13716
04.12.09
Kv3.1b Potassium Channel Monoclonal Antibody (Clone S16B-8)
For immunochemical detection of Kv3.1b
Antigen: fusion protein amino acids 437-585 of rat Kv3.1b · Clone designation: Mouse · Host: S16B-8 · Isotype: IgG1 · Application(s): WB and IHC ·
13717
04.12.09
Methylated Lysine Polyclonal Antibody-biotin
For immunochemical detection of methylated lysine
Antigen: methylated KLH · Host: rabbit · Application(s): WB, IP, and ELISA ·
13728
04.12.09
Methylated Lysine Polyclonal Antibody HRP Conjugate
For immunochemical detection of methylated lysine
Antigen: methylated KLH · Host: rabbit · Application(s): WB and ELISA ·
13729
04.12.09
Nav1.7 Sodium Channel Monoclonal Antibody (Clone S68-6)
For immunochemical detection of Nav1.7
Antigen: fusion protein amino acids 1,751-1,946 of rat Nav1.7 · Clone designation: S68-6 · Host: Mouse · Isotype: IgG1 · Application(s): WB, IP, and ICC ·
13718
04.12.09
Palmitoleic Acid-d14
An internal standard for the quantification of palmitoleic acid
An internal standard for the quantification of AEA by GC- or LC-mass spectrometry
9000431
04.12.09
Pseudolaric Acid B
Compound from traditional medicine with reported antifungal, anticancer actions
Pseudolaric acid B (PAB) is a diterpene acid isolated from the bark of P. kaempferi, a traditional Chinese medicinal plant. PAB has antifungal activities, consistent with its traditional use in the treatment of dermatological fungal infections. Moreover, PAB has diverse effects that are relevant to cancer therapy, including inducing apoptosis of cancer cells (IC50 = ~1 μM), preventing angiogenesis, and inhibiting tumor growth in vivo.
13527
04.12.09
SET7/9 Methyltransferase Inhibitor Screening Assay Kit
A convenient method for screening human SET7/9 inhibitors
Cayman’s SET7/9 Methyltransferase Inhibitor Screening Assay provides a convenient method for screening human SET7/9 inhibitors. The transfer of the methyl group from SAM by SET7/9 to the acceptor peptide (TAF 10) generates S-adenosylhomocysteine, which is rapidly converted to S-ribosylhomocysteine and adenine by adenosylhomocysteine nucleosidase. This rapid conversion prevents the buildup of adenosylhomocysteine and its feedback inhibition on the methylation reaction. Finally, the adenine is converted to hypoxanthine by adenine deaminase, which in turn is converted to urate and hydrogen peroxide (H2O2). The reaction between H2O2 and ADHP (10-acetyl-3,7-dihydroxyphenoxazine) produces the highly fluorescent compound resorufin. Resorufin fluorescence is analyzed using an excitation wavelength of 530-540 nm and an emission wavelength of 585-595 nm.
700270
04.12.09
TRPC4 Calcium Channel Monoclonal Antibody (Clone S77-15)
For immunochemical detection of TRPC4
Antigen: synthetic peptide amino acids 930-947 of rat TRPC4 · Clone designation: S77-15 · Host: Mouse · Isotype: IgG2b · Application(s): WB, IP, and ICC ·
13719
04.12.09
TRPM7 Channel (Ser/Thr Kinase) Monoclonal Antibody (Clone S74-25)
For immunochemical detection of TRPM7
Antigen: fusion protein amino acids 1,817-1,863 of murine TRPM7 · Clone designation: S74-25 · Host: Mouse · Isotype: IgG1 · Application(s): WB, IP, and ICC ·
13720
04.12.09
TRPV3 Calcium Channel Monoclonal Antibody (Clone S15-4)
For immunochemical detection of TRPV3
Antigen: amino acids 458-474 of rat TRPV3 · Clone designation: S15-4 · Host: Mouse · Isotype: IgG2a · Application(s): WB, IP, and ICC ·
13721
04.12.09
Ubiquitin Monoclonal Antibody (Clone 5B9-B3)
For immunochemical detection of ubiquitin
Antigen: native bovine ubiquitin conjugated to KLH · Clone designation: 5B9-B3 · Host: Mouse · Isotype: IgG2aκ · Application(s): WB and ELISA ·
13722
04.12.09
Ubiquitin Monoclonal Antibody (Clone 6C11-B3)
For immunochemical detection of ubiquitin
Antigen: native bovine ubiquitin conjugated to KLH · Clone designation: 6C11-B3 · Host: Mouse · Isotype: IgG2aκ · Application(s): WB and ELISA ·
13723
04.12.09
Ubiquitin Polyclonal Antibody
For immunochemical detection of ubiquitin
Antigen: native bovine ubiquitin conjugated to KLH · Host: rabbit · Application(s): WB, IP, and ChIP ·
13724
03.12.09
13,14-dihydro-16,16-difluoro Prostaglandin E1
Analog of PGE1
13,14-dihydro-16,16-difluoro PGE1 is an analog of PGE1. 13,14-dihydro PGE1 is a biologically active metabolite of PGE1, inhibiting platelet aggregation with comparable potency to the parent compound. The addition of two electron-withdrawing fluorine atoms, which should stabilize the molecule against hydrolytic cleavage, may be expected to delay degradation in vivo.
9000405
03.12.09
7(Z)-Pentacosene
Sex pheromone in Drosophila
7(Z)-Pentacosene is an unsaturated cuticular hydrocarbon that acts as a contact sex pheromone in fruit flies. In different species and genotypes of Drosophila, it can be found on both males and females. Pentacosene may stimulate copulation either by itself at high concentrations or when combined with other alkenes. Interestingly, the absolute level of pentacosene increases in Drosophila females immediately after copulation.
9000530
03.12.09
BIX01294 (hydrochloride hydrate)
An inhibitor of G9a histone methyltransferase
BIX01294 (hydrochloride hydrate) is a selective inhibitor of G9a HMTase (IC50 = 1.7 μM). It less effectively inhibits the HMTase G9a-like protein (GLP; IC50 = 38 μM) and has no effect on other known HMTases. BIX01294 has been used in combination with the calcium channel activator BayK8644 to facilitate the generation of induced pluripotent stem cells from somatic cells in vitro.
13124
03.12.09
(E)-Guggulsterone
A farnesoid X receptor antagonist
Guggulsterone, derived from resin of the guggul tree, is a competitive antagonist of FXR both in vitro and in vivo. The cis stereoisomer of guggulsterone, (E)-guggulsterone, decreases chenodeoxycholic acid (CDCA)-induced FXR activation with an IC50 value of 15 µM. By inhibiting CDCA-induced transactivation of FXR, guggulsterone lowers low-density lipoprotein cholesterol and triglyceride levels in rodents fed a high cholesterol diet.
10011296
03.12.09
(S)-HDAC-42
Inhibitor of HDACs
(S)-HDAC-42 is a potent inhibitor of HDACs (IC50 = 16 nM in vitro). It decreases the viability of prostate cancer cell lines (IC50 = 0.40 μM), increasing the expression of p21 and the acetylation of histone H3 while decreasing the phosphorylation of Akt and the expression of Bcl-XL. (S)-HDAC-42 also strongly suppresses the growth of PC-3 tumor xenografts, reducing levels of phospho-Akt and Bcl-XL protein in tumors.
13277
03.12.09
Soluble Epoxide Hydrolase Polyclonal Antibody
Antigen: murine recombinant soluble epoxide hydrolase · Host: rabbit · Application(s): WB ·
13560
03.12.09
XAV939
A tankyrase inhibitor
XAV939 is a potent, small molecule inhibitor of tankyrase (TNKS) 1 and 2 with IC50 values of 11 and 4 nM, respectively. By inhibiting TNKS activity, XAV939 increases the protein levels of the axin-GSK3β complex and promotes the degradation of β-catenin in SW480 cells. At concentrations as low as 0.33 µM, XAV939 inhibits colony formation of APC-deficient colorectal cancer cells.
13596
02.12.09
13,14-dihydro-15(R,S)-hydroxy-16,16-difluoro Prostaglandin E1-d4
An internal standard for the quantification of a PGE1 analog
It is intended for use as an internal standard for the quantification of 13,14-dihydro-15(R,S)-hydroxy-16,16-difluoro Prostaglandin E1 by GC- or LC-mass spectrometry (MS).
9000406
02.12.09
HCN4 Cyclic Nucleotide-gated Channel Monoclonal Antibody (Clone S114-10)
For immunochemical detection of HCN4
Antigen: fusion protein amino acids 1,019-1,108 (cytoplasmic C-terminus) of rat HCN4 · Clone designation: S114-10 · Host: Mouse · Isotype: IgG1 · Application(s): WB, ICC, and IHC ·
13709
02.12.09
KCNQ1 Potassium Channel Monoclonal Antibody (Clone S37A-10)
For immunochemical detection of KCNQ1
Antigen: fusion protein amino acids 2-101 of human KCNQ1 · Clone designation: S37A-10 · Host: mouse · Isotype: IgG1 · Application(s): WB, IP, IHC, and ICC ·
13711
02.12.09
KCNQ2 Potassium Channel Monoclonal Antibody (Clone S26A-23)
For immunochemical detection of KCNQ2
Antigen: fusion protein amino acids 1-59 of human KCNQ2 · Clone designation: S26A-23 · Host: Mouse · Isotype: IgG1 · Application(s): WB, IP, IHC, and ICC ·
13712
02.12.09
KCNQ4 Potassium Channel Monoclonal Antibody (Clone S43-6)
For immunochemical detection of KCNQ4
Antigen: fusion protein amino acids 2-77 of human KCNQ · Clone designation: S43-6 · Host: Mouse · Isotype: IgG1 · Application(s): WB, IP, and ICC ·
13713
02.12.09
Kir2.1 Potassium Channel Monoclonal Antibody (Clone S21-32)
For immunochemical detection of Kir2.1
Antigen: fusion protein amino acids 41-64 and 189-428 of murine Kir2.1 · Clone designation: S21-32 · Host: Mouse · Isotype: IgG1 · Application(s): WB and IHC ·
13714
02.12.09
Kir2.2 Potassium Channel Monoclonal Antibody (Clone S24-1)
For immunochemical detection of Kir2.2
Antigen: fusion protein amino acids 362-427 of murine Kir2.2 · Clone designation: S24-1 · Host: Mouse · Isotype: IgG1 · Application(s): WB and IHC ·
13715
02.12.09
S-Adenosylhomocysteine-d4
An internal standard for the quantification of SAH
S-Adenosylhomocysteine-d4 (SAH-d4) contains four deuterium atoms at the 3, 3’, 4, and 4’ positions. It is intended for use as an internal standard for the quantification of SAH by GC- or LC-mass spectrometry (MS).
9000372
01.12.09
CAY10616
Pro-apoptotic analog of resveratrol
CAY10616 is an analog of resveratrol which potently induces apoptosis in promyelocytic leukemia HL-60 cells (IC50 = 40 nM, vs. 50 μM for resveratrol). In addition, CAY10599 induces apoptosis (IC50 = 30 nM) in HL60R, a cell line derived from HL-60 that expresses a multidrug-resistance phenotype (resistant to daunorubicin, etoposide, and citarabine).
13291
01.12.09
HCN1 Cyclic Nucleotide-gated Channel Monoclonal Antibody (Clone S70-28)
For immunochemical detection of HCN1
Antigen: fusion protein amino acids 778-910 (cytoplasmic C-terminus) of rat HCN1 · Clone designation: S70-28 · Host: mouse · Isotype: IgG1 · Application(s): WB, IP, IHC, and ICC ·
13705
01.12.09
HCN2 Cyclic Nucleotide-gated Channel Monoclonal Antibody (Clone S71-37)
For immunochemical detection of HCN2
Antigen: fusion protein amino acids 761-863 (cytoplasmic C-terminus) of rat HCN2 · Clone designation: S71-37 · Host: Mouse · Isotype: IgG1 · Application(s): WB, IP, IHC, and ICC ·
13707
01.12.09
HCN3 Cyclic Neuclotide-gated Channel Monoclonal Antibody (Clone S141-28)
For immunochemical detection of HCN3
Antigen: fusion protein amino acids 660-779 (cytoplasmic C-terminus) of murine HCN3 · Clone designation: S141-28 · Host: Mouse · Isotype: IgG1 · Application(s): WB, ICC, and IHC ·
13708
01.12.09
N-Palmitoyl Glycine
An endogenous signaling lipid
N-palmitoyl glycine (PalGly) contains an 18-carbon saturated fatty acid that is amide-linked to glycine and is structurally similar to the phospholipid-derived N-acyl ethanolamines. Endogenously produced in rat skin and spinal cord, PalGly is present in 100-fold greater amounts in skin and 3-fold greater in brain compared to AEA. Injection of 0.43 µg PalGly in rat hindpaw inhibits heat-induced firing of nociceptive neurons in rat dorsal horn. PalGly treatment induces transient calcium influx in native dorsal root ganglion (DRG) cells and in the PTX-sensitive, DRG-like cell line F-11 (EC50 = 5.5 µM).
10009020
01.12.09
(Z)-Guggulsterone
A farnesoid X receptor antagonist
Guggulsterone, derived from resin of the guggul tree, is a competitive antagonist of FXR both in vitro and in vivo. The trans stereoisomer of guggulsterone, (Z)-guggulsterone, decreases chenodeoxycholic acid (CDCA)-induced FXR activation with an IC50 value of 17 µM. By inhibiting CDCA-induced transactivation of FXR, guggulsterone lowers low-density lipoprotein cholesterol and triglyceride levels in rodents fed a high cholesterol diet. While both cis and trans stereoisomers have been shown to directly decrease hepatic cholesterol, the Z isomer is the most studied. (Z)-Guggulsterone demonstrates antitumor-promoting effects inhibiting both constitutive and interleukin-6-induced STAT3 activation in human multiple myeloma cells and suppressing the VEGF-VEGF/R2-Akt signaling axis in DU145 human prostate cancer cells.
71800
25.11.09
GW 848687X
Antagonist of the PGE2 receptor EP1
GW 848687X is a potent and selective EP1 receptor antagonist (IC50 = 2.5 nM). It has >400-fold selectivity for EP1 relative to the other EP receptor subtypes, the PGD2 receptor, DP1, and the prostacyclin receptor, IP. GW 848687X has 30-fold selectivity over the thromboxane A2 receptor, TP, acting as a functional antagonist at this receptor at higher levels. Its actions against the FP and CRTH2/DP2 receptors have not been characterized. In vivo, GW 848687X has an excellent oral pharmacokinetic profile, with oral bioavailability at 54% in rats and 53% in dogs with a half-life of two hours in both species. In a rat model of chronic inflammatory joint pain, G W 848687X shows complete anti-hyperalgesic activity with an ED50 value of 1.3 mg/kg.
10010410
25.11.09
SET7/9 Polyclonal Antibody
For immunochemical analysis of SET7/9
Antigen: human SET7/9 amino acids 131-145 and 336-352 · Host: rabbit · Application(s): WB ·
13731
25.11.09
Sphingomyelinase Assay Kit
A sensitive tool for assaying neutral and acidic sphingomyelinase activity
Cayman’s Sphingomyelinase (SMase) Assay provides a simple, reproducible, and sensitive tool for assaying neutral and acidic sphingomyelinase activity from tissue homogenates, cell lysates, serum, saliva, and urine. The SMase Assay utilizes a coupled enzymatic reaction to monitor SMase activity. SMase hydrolyzes sphingomyelin to yield ceramide and phosphorylcholine. Alkaline phosphatase hydrolyzes phosphorylcholine forming choline. Choline is then oxidized by choline oxidase to yield betaine and H2O2. Finally, H2O2, in the presence of horseradish peroxidase (HRP), reacts with 10-acetyl-3,7-dihydroxyphenoxazine (ADHP) in a 1:1 stoichiometry to generate the highly fluorescent product resorufin. Resorufin fluorescence is analyzed with an excitation wavelength of 530-540 nm and an emission wavelength of 585-595 nm.
10006964
23.11.09
Toll-Like Receptor 12 Polyclonal Antibody
For immunochemical analysis of TLR12
Antigen: murine TLR12 amino acids 911-926 · Host: Rabbit · Application(s): WB and FC (intracellular) ·
13586
23.11.09
Toll-Like Receptor 7 Polyclonal Antibody
For immunochemical analysis of TLR7
Antigen: synthetic peptide from human TLR7 within the region of amino acids 706-728 · Host: rabbit · Application(s): WB, FC (intracellular and cell surface), IHC (frozen and paraffin), ICC, and IP ·
13591
16.11.09
BAY-41-8543
Stimulator of soluble guanylate cyclase
BAY-41-8543 is a heme-dependent stimulator of sGC, increasing the activity of recombinant sGC dose-dependently, from 0.1 nM to 100 μM, up to 92-fold. Surprisingly, NO donors synergize with BAY-41-8543 in stimulating recombinant sGC. BAY-41-8543 relaxes vessels and inhibits platelet aggregation in vitro at nM concentrations. In vivo, BAY-41-8543 decreases blood pressure dose-dependently, prolongs bleeding time, and reduces thrombosis. Inhalation of microparticles containing BAY-41-8543 increases pulmonary vasodilation without changing mean arterial pressure, suggesting that agonists of sGC may be efficacious in treating pulmonary hypertension.
10011131
16.11.09
YM-58483
Inhibitor of calcium release-activated calcium channels
YM-58483 is a potent inhibitor of CRAC channels, blocking thapsigargin-induced sustained calcium influx, Th2 cytokine production, and NF-AT-driven promoter activity in T lymphocytes (IC50 = 100 nM). YM-58483 also inhibits lung interleukin-4 and cysteinyl leukotriene generation as well as airway eosinophil infiltration in animal models of asthma.
13246
12.11.09
Cav1.3 Calcium Channel Monoclonal Antibody (Clone S48A-9)
For immunochemical detection of Cav1.3
Antigen: fusion protein amino acids 859-875 (N-terminal) of human Cav1.3 · Clone designation: S48A-9 · Host: mouse · Isotype: IgG2a · Application(s): WB, IHC, and ICC ·
13706
12.11.09
Cav3.2 Calcium Channel Monoclonal Antibody (Clone S55-10)
For immunochemical detection of Cav3.2
Antigen: fusion protein amino acids 1,019-1,293 (II-III loop) human Cav3.2 · Clone designation: S55-10 · Host: Mouse · Isotype: IgG1 · Application(s): WB, IHC, and ICC ·
13704
12.11.09
E-64
Irreversible cysteine protease inhibitor
E-64 is a natural, potent and irreversible inhibitor of cysteine proteases. Its IC50 values for inhibiting cathepsins K, S, and L, in vitro, are 1.4, 4.1, and 2.5 nM, respectively. E-64 also inhibits papain, calpain, and cathepsins B and H, but not serine proteases (e.g., plasmin, trypsin, tissue kallikrein) or aspartic proteases (e.g., pepsin). The mode of action involves the formation of a thioether linkage between E-64 and the thiol group of the protease; E-64 does not react with the functional thiol group of non-protease enzymes (e.g., creatine kinase, L-lactate hydrogenase). While E-64 is usually used in biochemical assays, it can also be used in intact cells at higher (μM) concentrations.
10007963
12.11.09
Toll-Like Receptor 10 Monoclonal Antibody (Clone 158C1114)
For immunochemical analysis of TLR10
Antigen: synthetic peptide from the extracellular domain of human TLR10 · Clone designation: 158C1114 · Host: Mouse · Isotype: IgG1 · Application(s): WB and FC (intracellular and cell surface) ·
13584
12.11.09
Toll-Like Receptor 11 Polyclonal Antibody
For immunochemical analysis of TLR11
Antigen: murine TLR11 amino acids 911-926 · Host: rabbit · Application(s): WB and FC (intracellular) ·
13585
11.11.09
ATF2 (Phospho-Thr69,71) Transcription Factor Assay Kit
96-Well assay for measurement of ATF2 (Phospho-Thr69,71)
Cayman’s ATF2 (Phospho-Thr69,71) Transcription Factor Assay is a non-radioactive, sensitive method for detecting specific transcription factor DNA binding activity in nuclear extracts. A 96-well enzyme-linked immunosorbent assay (ELISA) replaces the cumbersome radioactive electrophoretic mobility shift assay (EMSA). A specific double-stranded DNA (dsDNA) sequence containing the cAMP-response element (CRE) is immobilized onto the wells of a 96-well plate. ATF2 contained in a nuclear extract, binds specifically to the CRE. The activated ATF2 transcription factor complex is detected by addition of a specific primary antibody directed against the phospho-Thr69,71 epitope on ATF2. A secondary antibody conjugated to HRP is added to provide a sensitive colorimetric readout at 450 nm.
600130
11.11.09
Fumonisin B2
Inhibitor of sphingosine N-acyltransferase; mycotoxin; food contaminant
Fumonisin B2 is a mycotoxin originally isolated from F. moniliforme, a prevalent fungus of corn and other grains. Fumonisins cause food poisoning in livestock and humans following the consumption of Fusarium-infested corn. Fumonisin B2, like fumonisin B1 (Catalog No. 62580), structurally resembles sphingosine and, at 1 μM, inhibits sphingosine N-acyltransferase (>90%) in hepatocytes. Fumonisins induce apoptosis via altered sphingolipid metabolism, resulting in hepatotoxicity and nephrotoxicity. It is now known that fumonisins are produced by fungi other than F. moniliforme and occur as contaminants in a wide variety of foods.
13227
11.11.09
Taprostene (sodium salt)
Stable prostacyclin analog
Taprostene is a stable prostacyclin (PGI2) analog and agonist of the prostacyclin receptor, IP. It does not activate the PGE2 receptor EP4, which, like IP, promotes vascular smooth muscle relaxation when stimulated. Taprostene has been used extensively to study the role of the IP receptor in tissue preparations and in vivo. It has also been used in the screening and evaluation of potential IP antagonists.
10011348
10.11.09
DEPMPO-biotin
A biotinylated spin trap
DEPMPO-biotin is a biotinylated form of DEPMPO which retains the outstanding persistency of its adducts. The biotin moiety offers an effective means for monitoring biodistribution in cells, tissues, and organs when used with an avidin-conjugated reporter. Importantly, DEPMPO-biotin binds free radicals, such as S-nitroso groups, on proteins, producing adducts that can be analyzed via the biotin tag. This direct labeling of S-nitrosothiols (SNO) thus serves as an effective alternative to the more cumbersome biotin-switch method for monitoring SNO formation.
13251
10.11.09
Rhapontigenin
Natural resveratrol analog
Rhapontigenin is a natural analog of resveratrol with antioxidant and anti-cancer activity. It is a mechanism-based, selective inactivator of cytochrome P450 1A1 (IC50 = 400 nM), an aryl hydrocarbon hydroxylase which activates polycyclic aromatic hydrocarbons that act as procarcinogens. At higher concentrations, rhapontigenin inhibits the proliferation of Hep-G2 and HL-60R cancer cell lines (IC50 = 48 μM).
13293
09.11.09
G-418 Sulfate
Antibiotic used to select genetically-engineered cells
G-418 Sulfate is an aminoglycosidic antibiotic that is related to gentamicin. It is toxic to both prokaryotic and eukaryotic cells, as it blocks protein elongation during translation. G-418 is commonly used for the selection of cells that are genetically engineered with a plasmid containing the neo (neor) gene, which provides resistance to G-418. In mammalian cells, selection is commonly performed using 400 mg/L G-418, followed by 200 mg/L for culture maintenance; optimal concentrations may depend on cell type or plasmid and should be empirically determined.
13200
09.11.09
HDAC Cell-Based Activity Assay Kit
An easy tool for studying HDAC activity modulators in whole cells
Cayman’s HDAC Cell-Based Assay Kit provides an easy tool for studying HDAC activity modulators in whole cells. By using a cell-permeable HDAC substrate, the activity of various protein lysine-specific deacetylases including HDAC1-containing complexes can be measured in intact cells in a simple and homogenous manner. The fluorescence of the deacetylated reaction product can be analyzed using a plate reader or a fluorometer with excitation wavelengths of 340-360 nm and emission wavelengths of 440-465 nm. An HDAC inhibitor, trichostatin A (TSA), is included for checking specificity of the HDAC reaction. This assay parallels Cayman’s HDAC Activity Assay Kit (Catalog No. 10011563), which uses a nuclear extract rather than whole cells for the assay. Together, both assays will help to identify whether an inhibitor/activator has a direct effect on the enzyme.
600150
09.11.09
Toll-Like Receptor 8 Monoclonal Antibody (Clone 44C143)
For immunochemical analysis of TLR8
Antigen: synthetic peptide from human TLR8 within the region of amino acids 750-850 · Host: Mouse · Isotype: IgG1κ · Application(s): WB, FC (intracellular and cell surface), IHC (paraffin-embedded sections) ·
13592
09.11.09
Toll-Like Receptor 9 Monoclonal Antibody (Clone 26C593.2)
For immunochemical analysis of TLR9
Antigen: human TLR9 amino acids 268-284 · Clone designation: 26C593.2 · Host: Mouse · Isotype: IgG1κ · Application(s): WB, FC (intracellular and cell surface), IHC (frozen and paraffin-embedded sections), and ICC ·
13593
06.11.09
Agomelatine
A melatonin receptor agonist and 5-HT antagonist
Agomelatine is a metabolically stable analog of melatonin that displays agonist activity for MT1 and MT2 binding with nanomolar affinity. However, unlike melatonin, agomelatine is a competitive antagonist of human and porcine serotonin (5-HT2C) receptors (pKi = 6.2 and 6.4, respectively) as well as human 5-HT2B receptors (pKi = 6.6). Agomelatine abolishes 5-HT2C agonist effects both in cells and in vivo. It also dose-dependently increases extracellular levels of noradrenaline and dopamine in frontal cortex of freely moving rats.
13203
06.11.09
Quinestrol
A synthetic estrogen
Quinestrol is a synthetic estrogen that is effective in hormone replacement therapy. It is a 3-cyclopentyl ether of ethynyl estradiol. After gastrointestinal absorption, it is stored in adipose tissue, where it is slowly released and metabolized in the liver to its active form, ethinyl estradiol. Quinestrol has found limited use in suppressing lactation in postpartum women and, in combination with synthetic progestogens, as contraceptive therapy, although additional studies are needed for both applications.
10006320
05.11.09
13,14-dihydro-15-keto-tetranor Prostaglandin F1α
Potential metabolite of PGF1α and PGF2α
13,14-dihydro-15-keto tetranor Prostaglandin F1α is a potential metabolite of either PGF1α or PGF2α and likely precursor to tetranor-PGFM
13571
05.11.09
Cav1.2 Calcium Channel Monoclonal Antibody (Clone S57-46)
For immunochemical detection of Cav1.2
Antigen: fusion protein amino acids 1,507-1,733 · Clone designation: S-57-46 · Host: mouse · Isotype: IgG2b · Application(s): WB, IHC, ICC, and IF ·
13702
05.11.09
Cav1.3 Calcium Channel Monoclonal Antibody (Clone S38-8)
For immunochemical detection of Cav1.3
Antigen: fusion protein amino acids 2,025-2,161 (C-terminal) of rat Cav1.3 · Clone designation: S38-8 · Host: Mouse · Isotype: IgG1 · Application(s): WB, IHC, ICC, and IF ·
13703
05.11.09
Cavβ4 Calcium Channel Monoclonal Antibody (Clone S10-7)
For immunochemical detection of Cavβ1
Antigen: synthetic peptide from rat Cavβ4 amino acids 458-474 · Clone designation: S10-7 · Host: Mouse · Isotype: IgG1 · Application(s): WB, IHC, ICC, and IF ·
13701
05.11.09
DAz-2
A chemical probe for sulfenic acid detection
DAz-2 is a cell-permeable chemical probe that reacts specifically with sulfenic acid-modified proteins. The azido group of DAz-2 provides a method for selective conjugation to phosphine- or alkynyl- derivatized reagents, such as biotin or various fluorophores, for subsequent analysis of the labeled proteins. Use of DAz-2 in HeLa cells followed by Staudinger ligation to biotin and subsequesnt LC-MS/MS analysis, led to the identification 193 sulfenic acid-modified proteins having a diverse range of functions.
13382
05.11.09
MS-275
A histone deacetylase inhibitor
MS-275 is an inhibitor of histone deacetylases (HDACs) that preferentially inhibits HDAC1 (IC50 = 300 nM) over HDAC3 (IC50 = 8 μM). However, it does not inhibit HDAC8 (IC50 > 100 μM). MS-275 induces cyclin-dependent kinase inhibitor 1A (p21/CIP1/WAF1), slowing cell growth, differentiation, and tumor development in vivo. Recent studies suggest that MS-275 may be particularly useful as an antineoplastic agent when combined with other drugs, like adriamycin, inhibitors of poly (ADP-ribose) polymerase (PARP), or inhibitors of heat shock protein 90 (Hsp90).
13284
04.11.09
4-(n-nonyl) Benzeneboronic Acid
Potent inhibitor of FAAH
4-(n-Nonyl) benzeneboronic acid is a potent inhibitor of FAAH, with an IC50 of 9.1 nM. It is also able to inhibit monoacylglycerol lipase (MAGL), which hydrolyzes 2-arachidonoyl glycerol (2-AG), but at ~1000-fold higher concentration (IC50 = 7.9 μM).
13140
04.11.09
CAY10505
Inhibitor of PI3Kγ
CAY10505 is a potent inhibitor of PI3K, selectively inhibiting the γ isoform (IC50 = 30 nM) better than the α, β, and δ isoforms (IC50 = 0.94, 20, and 20 μM, respectively). Tested against a panel of 80 other kinases, CAY10505 significantly inhibits only the unrelated casein kinase 2 (CK2, IC50 = 20 nM). It also inhibits the phosphorylation of the PI3K substrate PKB/Akt in murine macrophages (IC50 = 228 nM). Oral administration of CAY10505 reduces neutrophil recruitment in mice to an extent that is comparable to that observed in PI3Kγ-deficient mice.
10009078
03.11.09
Palmitoleoyl 3-carbacyclic Phosphatidic Acid
Inhibitor of autotaxin
Palmitoleoyl 3-carbacyclic phosphatidic acid (3-ccPA 16:1) is a cyclic LPA analog that contains the 16:1 fatty acid, palmitoleate, at the sn-1 position of the glycerol backbone. At 25 μM, it inhibits the transcellular migration of MM1 cells across mesothelial cell monolayers in response to fetal bovine serum (86.9%) or LPA (99.9%) without affecting proliferation. 3-ccPA 16:1 significantly inhibits autotaxin (IC50 = 620 nM), an enzyme that is important in cancer cell survival, growth, migration, invasion and metastasis. When delivered intraperitoneally, 3-ccPA 16:1 significantly reduces the number of lung metastases formed in mice injected with B16F10 melanoma cells in the tail vein.
10010298
01.11.09
Toll-Like Receptor 2 Monoclonal Antibody (Clone TL2.1)
For immunochemical analysis of TLR2
Antigen: CHO cells transfected with human TLR2 cDNA · Clone designation: TL2.1 · Host: murine · Isotype: IgG2a · Application(s): WB, FC (intracellular and cell surface), ICC, IP, and IHC ·
13587
01.11.09
Toll-Like Receptor 6 Polyclonal Antibody
For immunochemical analysis of TLR6
Antigen: synthetic peptide from murine TLR6 · Host: rabbit · Application(s): WB and FC (intracellular) ·
13590
28.10.09
13,14-dihydro-15-keto-tetranor Prostaglandin D2
Potential metabolite of PGD2
13,14-dihydro-15-keto-tetranor PGD2 is a potential metabolite of PGD2. It would be produced from the known metabolite 13,14-dihydro-15-keto PGD2 (Catalog No. 12610), which is a known agonist for the CRTH2/DP2 receptor.
13100
28.10.09
Anhydrotetracycline (hydrochloride)
Regulator of TetR and revTetR transcriptional repressors
Anhydrotetracycline (hydrochloride) is a powerful effector in both the tetracycline repressor (TetR) and reverse TetR (revTetR) systems, binding the Tet repressor 35-fold more strongly than Tet. Moreover, anhydrotetracycline poorly binds the 30S ribosomal subunit, compared to Tet, so it does not act as a general inhibitor of translation and is a poor antibiotic. Perhaps related to this, the concentration of anhydrotetracycline that inhibits eukaryotic cell growth is more than a 1,000-fold above the dose that alters transcription through TetR.
10009542
28.10.09
FTY720 phenoxy-biotin
Biotin-tagged FTY720 analog
Biotin-FTY720 is a biotin-tagged analog of FTY720. The hydroxy methyl side chain of FTY720 that is targeted for phosphorylation by sphingosine kinases is retained in this analog, suggesting that it would likewise be phosphorylated in vivo.
13254
28.10.09
Ro 31-8220 (mesylate)
Inhibitor of protein kinase C
Ro 31-8220 is a potent, cell-permeable bisindolylmaleimide inhibitor of protein kinase C (PKC) isoforms (IC50 = 5, 24, 14, 27, and 24 nM for PKC-α, PKC-βI, PKC-βII, PKC-γ, and PKC-ε, respectively). It is a poor inhibitor of protein kinase A (PKA, IC50 = 0.9 μM) and calcium/calmodulin kinase II (IC50 = 17 μM). Ro 31-8220 also inhibits glycogen synthase kinase 3 (IC50 = 6.8 nM).
13334
27.10.09
IBMX
Non-specific inhibitor of cAMP and cGMP phosphodiesterases
IBMX is a widely-used non-specific inhibitor of cyclic AMP and cyclic GMP phosphodiesterases (PDEs) (IC50 = 19, 50, 18, 13, 32, 7, and 50 μM for PDE1, PDE2, PDE3, PDE4, PDE5, PDE7, and PDE11, respectively). PDE8A, PDE8B, and PDE9 are insensitive to IBMX. By inhibiting PDEs, IBMX increases cellular cAMP and cGMP levels, activating cyclic-nucleotide-regulated protein kinases. Methylxanthines, including IBMX, caffeine, and theophylline, bind adenosine receptors, typically antagonizing the suppressive effects of natural agonists.
13347
27.10.09
Toll-Like Receptor 3 Monoclonal Antibody (Clone 40C1285.6)
For immunochemical analysis of TLR3
Antigen: human TLR3 of amino acids 55-70 · Clone designation: 40C1285.6 · Host: mouse · Application(s): WB, FC (intracellular and cell surface), IP, IHC, and ICC ·
13588
27.10.09
Toll-Like Receptor 4 Monoclonal Antibody (Clone HTA125)
For immunochemical analysis of TLR4
Antigen: Ba/F3 cell line expressing human TLR4 cell surface antigen · Clone designation: HTA125 · Host: mouse · Isotype: IgG2aκ · Application(s): FC (intracellular and cell surface), IP, neutralization, and ICC ·
13589
27.10.09
Toll-Like Receptor 5 Monoclonal Antibody (Clone 85B152.5)
For immunochemical analysis of TLR5
Antigen: synthetic peptide corresponding to a portion of human TLR5 · Clone designation: 85B152.5 · Host: mouse · Isotype: IgG2a · Application(s): WB and FC (intracellular and cell surface) ·
13595
26.10.09
8-Isoprostane Express EIA Kit
A competitive assay for the quantification of 8-isoprostane
Limit of detection: 80% B/B0: 10 pg/ml · Sensitivity: 50% B/B0: 50 pg/ml · Cayman’s 8-Isoprostane Express EIA is a competitive assay that can be used for quantification of 8-isoprostane in plasma, serum, urine, whole blood, tissue culture supernatants, and other sample matrices. The EIA typically displays an IC50 (50% B/B0) of approximately 50 pg/ml and a detection limit (80% B/B0) of approximately 10 pg/ml.
516360
26.10.09
NMDA Receptor NR1 Subunit Monoclonal Antibody
For immunochemical detection of NMDA
Antigen: fusion protein containing amino acids 1-564 of the NR1 subunit of rat NMDA receptor · Host: murine · Application(s): IP and WB ·
10607
26.10.09
NMDA Receptor NR2A Subunit Polyclonal Antibody
For immunochemical detection of NMDA
Antigen: fusion protein from the C-terminus of the NR2A subunit of rat NMDA receptor · Host: rabbit · Application(s): IHC, IP, and WB ·
10608
26.10.09
NMDA Receptor NR2B Subunit Polyclonal Antibody
For immunochemical detection of NMDA
Antigen: fusion protein from the C-terminus of the NR2B subunit of rat NMDA receptor · Host: rabbit · Application(s): IHC, IP, and WB ·
10609
24.10.09
Cavβ1 Calcium Channel Monoclonal Antibody (Clone S7-18)
For immunochemical detection of Cavβ1
Antigen: synthetic peptide from rat Cavβ1 amino acids 19-34 · Clone designation: S7-18 · Host: Mouse · Isotype: IgG2a · Application(s): WB, IHC, and ICC ·
13700
23.10.09
13,14-dihydro-15-keto-tetranor Prostaglandin E2
Potential metabolite of PGE2
13,14-dihydro-15-keto tetranor PGE2 is a potential metabolite of PGE2. It would be produced from the known metabolite 13,14-dihydro-15-keto PGE2 (Catalog No. 14650), which is known to have a short plasma half-life.
13101
23.10.09
EX-527
Inhibitor of SIRT1
EX-527 is a cell-permeable, selective inhibitor of SIRT1 (IC50 = 98 nM). It inhibits other SIRTs only at much higher concentrations and has no effect on other HDACs. EX-527 has been used to investigate the relationship between SIRT1-mediated deacetylation of p53, p53 activity, and cell survival following DNA damage.
10009798
23.10.09
Nilotinib
A tyrosine kinase inhibitor
Nilotinib is a second generation tyrosine kinase inhibitor that is reported to have been used in targeted therapy for cancer. Specifically, it potently inhibits Bcr/Abl tyrosine kinase and is effective in the treatment of chronic myeloid leukemia (MLL) or Philadelphia chromosome acute lymphoblastic leukemia (Ph+ ALL), even in patients who are resistant to the first generation drug, imatinib (Gleevec). Nilotinib is ~20-fold more potent than imatinib in inhibiting both wild-type and mutant Bcr/Abl (e.g., IC50 = 15 versus 280 nM, respectively, for wild-type Bcr/Abl). Also, nilotinib regulates the gene expression for DNA helicase complex, cyclins, and cyclin-dependent kinases, inhibiting cell proliferation and decreasing progression through S phase, while imatinib does not.
10010422
23.10.09
Synapsin I Polyclonal Antibody
For immunochemical detection of Synapsin I
Antigen: native protein purified from bovine brain · Host: rabbit · Application(s): IF, IHC, IP, and WB ·
10606
23.10.09
Synapsin I Polyclonal Antibody (neat serum)
For immunochemical detection of Synapsin I
Antigen: native protein purified from bovine brain · Host: rabbit · Application(s): WB ·
10605
23.10.09
Tyrosine Hydroxylase Polyclonal Antibody
For immunochemical detection of Hydroxylase
Antigen: SDS-denatured rat tyrosine hydroxylase, purified from pheochromocytoma · Host: rabbit · Application(s): IF, IHC, and WB ·
10604
22.10.09
AGK2
Inhibitor of SIRT2
AGK2 is a cell-permeable, selective inhibitor of SIRT2 (IC50 = 3.5 μM) that minimally affects either SIRT1 or SIRT3 at 10-fold higher levels. It rescues dopamine neurons from α-synuclein toxicity in both in vitro and in vivo Parkinson’s disease models, mimicking the effect of siRNA-mediated blockade of SIRT2 expression. AGK2 may be a useful tool for studying the roles of SIRT2 in neurodegeneration and aging, as well as cell cycle progression and tumorigenesis.
13145
22.10.09
DARPP-32 (Phospho-Thr34) Polyclonal Antibody
For immunochemical detection of DARPP-32
Antigen: phosphopeptide corresponding to amino acid residues surrounding phospho-Thr34 of rat DARPP-32 · Host: rabbit · Application(s): WB ·
10603
22.10.09
GABAA Receptor δ subunit (N-Term) Polyclonal Antibody
For immunochemical detection of GABAA
Antigen: fusion protein from the N-terminus of the δ-subunit of rat GABAA receptor · Host: rabbit · Application(s): WB, IHC, and IP ·
10600
22.10.09
GluR1 (Phospho-Ser831) Polyclonal Antibody
For immunochemical detection of GluR1
Antigen: phosphopeptide corresponding to amino acid residues surrounding the phospho-Ser831 of GluR1 · Host: rabbit · Application(s): WB ·
10602
22.10.09
GluR1 (Phospho-Ser845) Polyclonal Antibody
For immunochemical detection of GluR1
Antigen: phosphopeptide corresponding to amino acid residues surrounding the phospho-Ser845 of GluR1 · Host: rabbit · Application(s): IHC and WB ·
10601
22.10.09
Monoacylglycerol Lipase Inhibitor Screening Assay Kit
A colorimetric method for screening MGL inhibitors
Cayman’s Monoacylglycerol Lipase (MAGL) Inhibitor Screening Assay provides a convenient method for screening human MAGL inhibitors. MAGL hydrolyzes 4-nitrophenylacetate resulting in a yellow product, 4-nitrophenol, with an absorbance of 405-412 nm.
705192
21.10.09
GSK264220A
An endothelial lipase inhibitor
GSK264220A is a potent inhibitor of endothelial lipase (IC50 = 16 nM). Levels of HDL cholesterol are inversely correlated with endothelial lipase protein activity. Therefore, inhibition of endothelial lipase by compounds like GSK264220A may be expected to increase HDL levels and potentially decrease the risk of cardiovascular disease.
13009
21.10.09
Rapamycin
Immunosuppressant that blocks mTORC1 signaling
Rapamycin is an immunosuppressant that is used primarily to prevent the rejection of organ and bone marrow transplant. It was first described as a potent inhibitor of IL-2 activation of lymphocytes (IC50 = 5 pM). It is now known that rapamycin specifically interacts with the cytosolic FK-binding protein 12 (FKBP12) to form a complex which inhibits the mammalian target of rapamycin (mTOR) pathway by directly binding to mTOR Complex 1 (mTORC1). Rapamycin and other inhibitors of mTORC1 signaling show potential in treating cancer, adipogenesis, diabetes, tuberous sclerosis, and cardiovascular disease.
13346
21.10.09
Valproic Acid (sodium salt)
HDAC inhibitor with numerous in vivo applications
Valproic acid is an analog of the natural fatty acid valeric acid. The sodium salt of valproic acid has long been used as an anticonvulsant to prevent many kinds of seizures. It is an inhibitor of histone deacetylases (HDACs), inhibiting Class I HDACs with an IC50 of ~ 2 mM. Valproic acid also inhibits glycogen synthase kinase (GSK3) and depletes cellular inositol-1,4,5-trisphosphate (IP3). Because of these actions, valproic acid shows promise in combination therapy for cancer and in treating Alzheimer’s disease. Valproic acid (1 mM) also has pronounced effects on stem cell differentiation and self-renewal.
13033
15.10.09
L-655,240
Potent antagonist of the thromboxane A2 receptor
L-655,240 is a potent antagonist of the TP receptor in vitro (IC50 = 7 nM). It also is effective at blocking TP-mediated bronchoconstriction in vivo and platelet aggregation ex vivo. Whether the two TP isoforms differ in their sensitivity to L-655,240 is not known.
10011562
14.10.09
IM-54
Inhibitor of H2O2-induced necrotic cell death
IM-54 is an indolylmaleimide derivative which, at 1 μM, inhibits necrotic cell death induced by H2O2 in promyelocytic leukemia HL-60 cells. It does not prevent etoposide-induced apoptosis and does not inhibit protein kinase C or S6 kinase 1.
13323
14.10.09
Oleoyl 3-carbacyclic Phosphatidic Acid
Inhibitor of autotaxin, antagonist of LPA1 and LPA3
Oleoyl 3-carbacyclic phosphatidic acid (3-ccPA 18:1) is a cyclic LPA analog that contains the 18:1 fatty acid, oleate, at the sn-1 position of the glycerol backbone. At 25 μM, it inhibits the transcellular migration of MM1 cells across mesothelial cell monolayers in response to fetal bovine serum (90.1%) or LPA (99.9%) without affecting proliferation. 3-ccPA 18:1, at 0.1-1.0 μM, significantly inhibits autotaxin, an enzyme that is important in cancer cell survival, growth, migration, invasion, and metastasis.
10010299
12.10.09
16-phenoxy tetranor Prostaglandin F2α cyclopropyl methyl amide
An analog of PGF2α
16-phenoxy tetranor prostaglandin F2α cyclopropyl methyl amide (16-phenoxy tetranor PGF2α cyclopropyl methyl amide) is an analog of PGF2α containing a 16-phenoxy group on the lower (ω) side chain and a cyclopropyl methyl amide at the C-1 position. There are no published reports on the biological activity of 16-phenoxy tetranor PGF2α cyclopropyl methyl amide.
10010809