A CDK inhibitor
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].
参考文献:
[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
动态评分
0.0