Thapsigargin

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). 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. Thapsigargin shows anti-inflammatory and anti-cancer effects. References: (1) S.A. Patkar, et al., Agents Actions 9, 53 (1979) , (2) H. Hakii, et al., J. Cancer. Res. Clin. Oncol. 111, 177 (1986) , (3) Y. Sagara, & G. Inesi, J. Biol. Chem. 266, 13503 (1991) , (4) A. Tsukamoto & Y. Kaneko, Cell Biol. Int. 17, 969 (1993) , (5) J.P. Beaver & P. Waring, Cell Death Differ. 3, 415 (1996) , (6) M. Treiman, et al., Trends Pharmacol. Sci. 19,131 (1998) , (7) B. Tombal, et al., Prostate 43, 303 (2000) , (8) S.B. Christensen, et al., Anticancer Agents Med. Chem. 9, 276 (2009) , (9) N.T. Quynh Doan & S.B. Christensen, Curr. Pharm. Des. 21, 5501 (2015) (Review) , (10) N.T. Doan, et al., Steroids 97, 2 (2015) (Review) , (11) A. Jaskulska, et al., Int. J. Mol. Sci. 22, 4 (2020) (Review) Appearance: White crystalline powder. Solubility: Soluble in methanol, ethanol or DMSO. Identity: Determined by 1H-NMR. Declaration: Manufactured by Chemodex. Inchi Key: IXFPJGBNCFXKPI-IVRBKYRWSA-N Smiles: O=C1OC2C3=C(C)[C@@H](OC(/C(C)=C\C)=O)[C@@H](OC(CCCCCCC)=O)[C@]3([H])[C@](C)(OC(C)=O)C[C@@H](OC(CCC)=O)[C@]2(O)[C@@]1(O)C