Chemical Name:9-Hydroxy-4-phenyl-pyrrolo[3,4-c]carbazole-1,3(2H,6H)-d
ione
Biological Activity:
Selective inhibitor of checkpoint kinases Chk1
and Wee1 (IC50 values are 47 and 97 nM respectively). Displays
selectivity over a range of other protein kinases; IC50 values are
3.4, 3.75, > 5, > 50, > 50 and > 50 μM for PKC,
CDK4, other CDKs, c-Src, PDGFR and FGFR respectively.
Squireet al
(2005) Structure and inhibition of the human cell cycle checkpoint kinase,
Wee1A kinase: an atypical tyrosine kinase with a key role in CDK1 regulation.
Structure 13 541. Palmeret al (2006)
4-Phenylpyrrolo[3,4-c]carbazole-1,3(2H,6H)-dione
inhibitors of the checkpoint kinase Wee1. Structure-activity relationships for
chromophore modification and phenylring substitutions. J.Med.Chem. 49
4896.