CGP74514A

481724-82-7

Others, Apoptosis, CDK

Apoptosis, Others, Cell Cycle/Checkpoint

CGP74514A is a CDK1 inhibitor with potential anticancer activity. In U937 cells, CGP74514A - induced apoptosis (5 microM) became apparent within 4 hr and approached 100% by 24 hr. The pan- caspase inhibitor Boc-fmk and the caspase-8 inhibitor lETD-fmk opposed CGP74514A -induced caspase-9 activation and PARP degradation, but not cytochrome c or Smac/DIABLO release. CGP74514A -mediated apoptosis was substantially blocked by ectopic expression of full-length Bel- 2, a loop-deleted mutant Bcl-2, and Bcl-x (L) . CGP74514A treatment (5 microM; 18 hr) resulted in increased p21 (CIP1) expression, p27 (KIP1) degradation, diminished E2F1 expression, and dephosphorylation of p34 (CDC2) . It also induced early (i.e., within 2 hr) inhibition of CDK1 activity and dephosphorylation of pRb, followed by pRb degradation, but did not block pRb phosphorylation at CDK2- and CDK4- specific sites. These findings indicate that the selective CDK1 inhibitor, CGP74514A , induces complex changes in cell cycle......

N(C1=C2C(N(CC)C=N2)=NC(N[C@@H]3[C@H](N)CCCC3)=N1)C4=CC(Cl)=CC=C4.Cl

C19H25Cl2N7

422.36

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