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Description: Kenpaullone (NSC-664704) is a novel, potent and ATP competitive inhibitor of CDK1/cyclin B and GSK-3beta, with IC50s of 0.4 uM and 23 nM, and also inhibits CDK2/cyclin A, CDK2/cyclin E, and CDK5/p25 with IC50s of 0.68 uM, 7.5 uM, 0.85 uM, respectively. Kenpaullone acts by competitive inhibition of ATP binding. Molecular modeling indicates that kenpaullone can bind in the ATP binding site of CDK2 with residue contacts similar to those observed in the crystal structures of other CDK2-bound inhibitors.
References: Cancer Res. 1999 Jun 1; 59(11):2566-9.; Proc Natl Acad Sci U S A. 2009 Jun 2; 106(22):8912-7.
Related CAS#:237430-03-4 (Alsterpaullone)
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