Chemical Name: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]de
c-7-yl]-1-propenyl]-2-oxazoly]butyl
Biological Activity:
Potent and selective cell-permeable inhibitor of protein
phosphatase 1 (IC50 = 0.3-0.7 nM) and protein phosphatase 2A (IC50
= 0.5-1 nM). Displays > 10,000,000-fold selectivity over PP2B and PP2C.
Ishiharaet al (1989) Calyculin A and okadaic acid: inhibitors of
protein phosphatase activity. Biochem.Biophys.Res.Comm. 159 871. Favreet al (1997) Differential inhibition and posttranslational modification
of protein phosphatase 1 and 2A in MCF7 cells treated with calyculin-A, okadaic
acid, and tautomycin. J.Biol.Chem. 272 13856. Lindval et
al (1997) The binding mode of calyculin A to protein phosphatase-1.
J.Biol.Chem. 272 23312. McCluskeyet al (2002)
Serine-threonine protein phosphatase inhibitors: development of therapeutic
strategies. J.Med.Chem. 45 1151.
