cgp74514 dihydrochloride

Potent cdk1 inhibitor (IC50 = 25 nM). Reduces Akt phosphorylation and increases mitochondrial damage in leukemia cells in vitro in combination with LY 294002. Yu et al (2013) The lethal effects of pharmacological cyclin-dependent kinase inhibitors in human leukemia cells proceed through a phosphatidylinositol 3-kinase/Akt-dependent process. Cancer Res. 63 1822 PMID:12702569 |Furet et al (2000) Structure-based design of potent CDK1 inhibitors derived from olomoucine. J.Comput.Aided Mol.Des. 14 403 PMID:10896313

CGP-74514 dihydrochloride 是一种具有高度选择性的细胞周期蛋白依赖性激酶 1 (CDK1) 抑制剂 (IC50=25 nM)。它能够抑制 CDK1/细胞周期蛋白 B 复合物的活性，导致细胞周期停滞于 G2/M 期，并诱导肿瘤细胞的凋亡 (apoptosis)。此化合物在膀胱癌研究中展现出潜力。