General Description
A cell-permeable quinolinyl thiazolinone compound that acts as a potent and ATP-competitive inhibitor of Cdk1 (K
i = 35 nM and 110 nM for Cdk1/B1 and Cdk1/A, respectively). It affects Cdk2/E, PKCδ, and SGK only at much higher concentrations (K
i = 340, 318, and 497 nM, respectively), and shows little effect against Cdk4/D and six other commonly studied kinases (K
i =2 M). Short-term treatment for up to 20 hrs results in fully reversible G2/M cell cycle arrest, while prolonged treament (>48 hrs) results in apoptotic cell death in proliferating cancer cells, but not in nontumorigenic epithelial cell lines. The solid form of this compound (Cat. No.
217699) is also available.
