CGP74514A New

Data Sheet For research use only. Not for human use.

Cat. No. ：BCP20240CAS No. ：190653-73-7Purity：98%

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CAS No.	190653-73-7	Cat. No.	BCP20240
Name	CGP74514A
Synonyms	CGP-74514A; CGP 74514A;
SMILES	CCN1C=NC2=C1N=C(N=C2NC3=CC(=CC=C3)Cl)NC4CCCCC4N
Chemical Name
Formula	C19H24ClN7	M. Wt	385.89
Purity	98%	Storage	Store at 4-8°C
Description	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-related proteins in human leukemia cells accompanied by extensive mitochondrial damage, caspase activation, and apoptosis.