CGP60474

Short Summary : CDKs and PKC inhibitor, potent

Category : Cell Cycle/Checkpoint|Cyclin-Dependent Kinases

Purity : 0.98

CAS Number : 164658-13-3

Formula : C18H18ClN5O

Molecular Weight : 355.82

SMILE : C1=CC(=CC(=C1)Cl)NC2=NC=CC(=N2)C3=CC(=NC=C3)NCCCO

Solubility : Soluble in DMSO

Storage : Store at -20°C

Description : CGP60474 is a potent inhibitor of cyclin-dependent kinases (CDKs) with IC50 value of 17 nM for CDK1 [1]. It is also an inhibitor of Protein Kinase C (PKC) [1].CDKs are a family of protein kinases regulating the cell cycle. PKC plays an important role in signal transductions, cellular proliferation and differentiation [2].CGP60474 was highly selective for PKC than other serine/threonine and tyrosine kinases and showed competitive kinetics relative to ATP [2].References:[1]. Kuo GH, Deangelis A, Emanuel S, et al. Synthesis and identification of [1,3,5]triazine-pyridine biheteroaryl as a novel series of potent cyclin-dependent kinase inhibitors. J Med Chem, 2005, 48(14): 4535-4546.[2]. Stanetty P, Hattinger G, Schnürch M, et al. Novel and efficient access to phenylamino-pyrimidine type protein kinase C inhibitors utilizing a Negishi cross-coupling strategy. J Org Chem, 2005, 70(13): 5215-5220

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