| 化学名 | N-[(3S)-[4-(1E)-3-[(2R,3R,4R,7S,8S,9R)-2-[(1S,3S,4S,5R,7E,9E,11E,13Z)-14-Cyano-3,5-dihydroxy-1-methoxy-4,6,8,9,13-pentamethyl-7,9,11,13-tetradecatetraenyl]-9-hydroxy-4,4,8-trimethyl-3-(phosphonooxy)-1,6-dioxaspiro[4.5]dec-7-yl]-1-propenyl]-2-oxazoly]butyl |
| 产品描述 | Calyculin A is a natural, cell-permeable inhibitor of the serine-threonine protein phosphatases (PP) PP1 and PP2A (IC50s = 0.3-0.7 and 0.5-1 nM, respectively).[1],[2],[3] It is without significant effect against PP2B, PP2C, and PP4.[2] Through its effects on PP1 and PP2A, calyculin A has been shown to either promote or inhibit cancer cell growth in tumor cell lines and animal models.[4],[5] Reference:
[1]. Ishihara, H., Martin, B.L., Brautigan, D.L., et al. Calyculin A and okadaic acid: Inhibitors of protein phosphatase activity. Biochem. Biophys. Res. Commun. 159(3), 871-877 (1989).
[2]. McCluskey, A., Sim, A.T.R., and Sakoff, J.A. Serine-threonine protein phosphatase inhibitors: Development of potential therapeutic strategies. Journal of Medicinal Chemistry 45(6), 1151-1175 (2002).
[3]. Lindvall, M.K., Pihko, P.M., and Kosikinen, A.M.P. The binding mode of calyculin A to protein phosphatase-1. A novel spiroketal vector model. J. Biol. Chem. 272(37), (1997).
[4]. Fujiki, H., Suganuma, M., Yoshizawa, S., et al. Mechanisms of action of okadaic acid class tumor promoters on mouse skin. Environ. Health Perspect. 93, 211-214 (1991).
[5]. Zheng, Y.G., Wu, J., Chen, Z., et al. Chemical regulation of epigenetic modifications: Opportunities for new cancer therapy. Medicinal Research Reviews 28(5), 645-687 (2008). |
