PHA-793887

PHA-793887 is an inhibitor of cyclin-dependent kinases (CDKs, IC50s = 8, 8, 5, and 10 nM for Cdk2/cyclin A, Cdk2/cyclin E, Cdk5/p25, and Cdk7/cyclin H, respectively). It is selective for these CDKs over Cdk1/cyclin B, Cdk4/cyclin D1, Cdk9/cyclin T1, and glycogen synthase kinase 3beta (GSK3beta, IC50s = 60, 62, 138, and 79 nM, respectively), as well as a panel of 36 other kinases at 10 µM. PHA-793887 inhibits the proliferation of A2780 ovarian, HCT116 colon, and BxPC-3 pancreatic cancer cells (IC50s = 88, 163, and 3,444 nM, respectively). It inhibits reactivation of latent HIV-1 induced by prostratin (Cay-10272), panobinostat (Cay-13280), or JQ-1 in 24ST1NLESG cells (IC50s = 0.004, 0.0082, and 0.016 µM, respectively). PHA-793887 (20 mg/kg) reduces tumor growth and increases survival in HL-60 and K562 leukemia mouse xenograft models.Formal Name: 3-methyl-N-[1,4,5,6-tetrahydro-6,6-dimethyl-5-[(1-methyl-4-piperidinyl)carbonyl]pyrrolo[3,4-c]pyrazol-3-yl]-butanamide. CAS Number: 718630-59-2. Molecular Formula: C19H31N5O2. Formula Weight: 361.5. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, Ethanol: 30 mg/ml, Ethanol:PBS(pH 7.2) (1:1): 0.5 mg/ml. lambdamax: 235 nm. SMILES: CN1CCC(C(N2C(C)(C)C(NN=C3NC(CC(C)C)=O)=C3C2)=O)CC1. InChi Code: InChI=1S/C19H31N5O2/c1-12(2)10-15(25)20-17-14-11-24(19(3,4)16(14)21-22-17)18(26)13-6-8-23(5)9-7-13/h12-13H,6-11H2,1-5H3,(H2,20,21,22,25). InChi Key: HUXYBQXJVXOMKX-UHFFFAOYSA-N.