10522  Thapsigargin

(CAS 67526-95-8)




In cells, sarco/endoplasmic calcium ATPases (SERCAs) transport free calcium into the sarcoplasmic and endoplasmic reticula, lowering intracellular calcium levels to stop signaling through this cation. Thapsigargin is a non-competitive, cell permeable inhibitor of calcium transport by SERCAs (IC50 values are cell type-dependent and range from ~2-80 nM).1,2 Inhibition of SERCAs leads to an increase in intracellular calcium, which has been linked to cell activation, release of histamine from mast cells, and increased proliferation of certain types of cancer cells.1,3,4 In vivo, thapsigargin and related sesquiterpene lactones have anti-inflammatory and anti-cancer effects.5,6
1  Sabala, P., Czarny, M., Woronczak, J.P., et al. Thapsigargin: Potent inhibitor of Ca2+ transport ATP-ases of endoplasmic and sarcoplasmic reticulum. Acta Biochim Pol 40(3) 309-319 (1993).
2  Treiman, M., Caspersen, C., and Christensen, S.B. A tool coming of age: Thapsigargin as an inhibitor of sarco-endoplasmic reticulum Ca2+-ATPases. Trends Pharamacol Sci 19(4) 131-135 (1998).
3  Ali, H., Christensen, S.B., Foreman, J.C., et al. The ability of thapsigargin and thapsigargicin to activate cells involved in the inflammatory response. Br J Pharmacol 85(3) 705-712 (1985).
4  Jackson, T.R., Patterson, S.I., Thastrup, O., et al. A novel tumour promoter, thapsigargin, transiently increases cytoplasmic free Ca2+ without generation of inositol phosphates in NG115-401L neuronal cells. Biochem J 253(1) 81-86 (1988).
5  Christensen, S.B., Skytte, D.M., Deanmeade, S.R., et al. A Trojan horse in drug development: Targeting of thapsigargins towards prostate cancer cells. Anticancer Agents Med Chem 9(3) 276-294 (2009).
6  Ghantous, A., Gali-Muhtasib, H., Saliba, N.A., et al. What made sesquiterpene lactones reach cancer clinical trials? Drug Discov Today 15(15-16) 668-678 (2010).

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1 mg €66.00
5 mg €264.00
Pricing updated 2014-10-01.
Prices are subject to change without notice.