Chemical Name:2-[1-(3-Dimethylaminopropyl)indol-3-yl]-3-(indol-3-yl)
maleimide
Biological Activity:
Very potent and selective inhibitor
of protein kinase C, selective for the α
and β1 isoforms (IC50 values are 0.0084, 0.0180, 0.210, 0.132, and
5.8 μM for α, β1,
δ, e, and z isoforms
respectively). Selective over MLCK, PKG and PKA (IC50 values are
0.6, 4.6, and 33 μM respectively). Potent
antagonist at the 5-HT3 receptor (Ki = 29.5 nM).
Anti-inflammatory in vivo.
Toullecet al (1991) The bisindolylmaleimide GF 109203X is a
potent and selective inhibitor of protein kinase C. J.Biol.Chem. 266 15771.
Martiny-Baronet al (1993) Selective inhibition of protein kinase
C isozymes by the indolocarbazole Go 6976. J.Biol.Chem. 268 9194.
Jacobsonet al (1995) Anti-inflammatory properties of Go 6850: a
selective inhibitor of protein kinase C. J.Pharmacol.Exp.Ther. 275
995. Coultrapet al (1999) Competitive antagonism of the mouse
5-hydroxytryptamine3 receptor by bisindolylmaleimide I, a ''selective'' protein kinase
C inhibitor. J.Pharmacol.Exp.Ther. 290 76.