Chemical Name:(9R,10S,12S)-2,3,9,10,11,12-Hexahydro-10-hydroxy-9-meth
yl-1-oxo-9,12-epoxy-1H-diindolo[1,2,3-fg:3',2',1'-kl]py
rrolo[3,4-i][1,6]benzodiazocine-10-carboxylic acid,
hexyl ester
Biological Activity:
Potent, selective inhibitor of protein kinase A (Ki =
60 nM). Has no effect on PKG or PKC (Ki > 2 μM). Reversibly arrests human skin fibroblasts in the G1
phase.
Kaseet al (1987) K-252 compounds, novel and potent inhibitors
of protein kinase C and cyclic nucleotide-dependent protein kinases.
Biochem.Biophys.Res.Comm. 142 436. Gadboiset al
(1992) Multiple kinase arrest points in the G1 phase of
nontransformed mammalian cells are absent in transformed cells.
Proc.Natl.Acad.Sci.USA 89 8626. Cabellet al (1993)
Effects of selective inhibition of protein kinase C, cyclicAMP-dependent
protein kinase, and Ca(2+)-calmodulin-dependent protein kinase on neurite
development in cultured rat hippocampal neurons. Int.J.Dev. Neurosci. 11
357.