产品描述:
P276-00 is an inhibitor of cyclin-dependent kinase 9 (Cdk9), Cdk4, and Cdk1 (IC50s = 0.020, 0.063, and 0.079 µM, respectively).{68654} It is selective for these CDKs over Cdk2/cyclin E, Cdk2/cyclin A, Cdk6, and Cdk7 (IC50s = 2.54, 0.224, 0.396, and 2.87 µM, respectively), as well as a panel of eight other kinases. P276-00 (1 µM) induces apoptosis in HL-60 leukemia cells. It induces cell cycle arrest at the G1 phase in synchronized H460 non-small cell lung cancer (NSCLC) cells when used at concentrations of 1.5 and 5 µM.{68655} P276-00 (50 mg/kg once per day) reduces tumor volume in an H460 mouse xenograft model. It also inhibits reactivation of latent HIV-1 induced by the HIV re-activator prostratin (Item No. 10272), pan-HDAC inhibitor panobinostat (Item No. 13280), or bromodomain inhibitor JQ-1 in 24ST1NLESG cells (IC50s = 0.1, 0.07, and 0.075 µM, respectively).{54093}