Chemical Name:(9S, 10R,
12R)-2,3,9,10,11,12-Hexahydro-10-methoxy-2,9-dimethyl-1
-oxo-9,12-epoxy-1H-diindolo[1,2,3-fg:3',2',1'-kl]pyrrol
o[3,4-i][1,6]benzodiazocine-10-carboxylic acid, methyl
ester
Biological Activity:
Selective inhibitor of protein kinase G (Ki values are
0.23, 4 and > 10 μM for inhibition of PKG,
PKC and PKA respectively). Inhibits SNP-stimulated PKG activity with an IC50
of 60 nM in dispersed smooth muscle cells and has little effect on PKA activity
at concentrations of up to 10 μM.
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. Murthy and Makhlouf (1995)
Interaction of cA-kinase and cG-kinase in mediating relaxation of dispersed
smooth muscle cells. Am.J.Physiol. 268 C171. Smolenskiet
al (1998) Functional analysis of cGMP-dependent protein kinases I and II as
mediators of NO/cGMP effects. Naunyn-Schmied.Arch.Pharmacol. 358
134.