P276-00 (hydrochloride)

P276-00 is an inhibitor of cyclin-dependent kinase 9 (Cdk9), Cdk4, and Cdk1 (IC50s = 0.020, 0.063, and 0.079 µM, respectively). 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. 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 (Cay-10272), pan-HDAC inhibitor panobinostat (Cay-13280), or bromodomain inhibitor JQ-1 in 24ST1NLESG cells (IC50s = 0.1, 0.07, and 0.075 µM, respectively).Formal Name: 2-(2-chlorophenyl)-5,7-dihydroxy-8-[(2R,3S)-2-(hydroxymethyl)-1-methyl-3-pyrrolidinyl]-4H-1-benzopyran-4-one, monohydrochloride. CAS Number: 920113-03-7. Synonyms: Riviciclib. Molecular Formula: C21H20ClNO5 . HCl. Formula Weight: 438.3. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: Acetonitrile: Soluble, DMSO: Soluble. SMILES: OC1=CC(O)=C(C(C=C(C2=CC=CC=C2Cl)O3)=O)C3=C1[C@@H]4CCN([C@H]4CO)C.Cl. InChi Code: InChI=1S/C21H20ClNO5.ClH/c1-23-7-6-12(14(23)10-24)19-15(25)8-16(26)20-17(27)9-18(28-21(19)20)11-4-2-3-5-13(11)22,/h2-5,8-9,12,14,24-26H,6-7,10H2,1H3,1H/t12-,14+,/m1./s1. InChi Key: OOVTUOCTLAERQD-OJMBIDBESA-N.