Staurosporine is a potent inhibitor of p34cdc2 and p34cdc2-like kinases.
We previously demonstrated that nontransformed cells arrest in the G1 phase of the cell cycle when treated with low concentrations (21 nM) of staurosporine (1). Both normal and transformed cells are blocked in the G2 phase of the cell cycle when treated with higher concentrations (160 nM) of staurosporine (1,2). In the present study, we show that staurosporine inhibits the activity of fractionated p34cdc2 and p34cdc2-like kinases with IC50 values of 4-5 nM. We propose that the G2 phase arrest in the cell cycle caused by staurosporine is due, at least in part, to the inhibition of the p34cdc2 kinases.
Gadbois
D M
DM
Life Sciences Division, Los Alamos National Laboratory, New Mexico 87545.
Hamaguchi
J R
JR
Swank
R A
RA
Bradbury
E M
EM
D000470:Alkaloids / Q000494:pharmacology*; D000595:Amino Acid Sequence; D000818:Animals; D016203:CDC2 Protein Kinase / Q000037:antagonists & inhibitors* / Q000302:isolation & purification; D002460:Cell Line; D005260:Female; D016195:G2 Phase / Q000187:drug effects; D007700:Kinetics; D008325:Mammary Neoplasms, Experimental; D051379:Mice; D008969:Molecular Sequence Data; D010455:Peptides / Q000138:chemical synthesis; D047428:Protein Kinase Inhibitors; D011505:Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors*; D019311:Staurosporine; D013379:Substrate Specificity
D000470:Alkaloids; D010455:Peptides; D047428:Protein Kinase Inhibitors; D011505:Protein-Tyrosine Kinases; D016203:CDC2 Protein Kinase; D019311:Staurosporine