CPI-455

CPI-455 is an inhibitor of the lysine demethylase 5 family (KDM5A-D). CPI-455 binds to the demethylase active site and selectively inhibits KDM5A-D (IC50s = 2-10 nM) over KDM2-4, 6, and 7 family members (IC50s = 1 to >25 µM). It increases histone H3K4me2/3 methylation in vitro and decreases the number of drug-tolerant cells in PC9 non-small cell lung, M14 melanoma, and SKBR3 breast cancer cell populations. CPI-455 also reduces growth of glioblastoma cells resistant to temozolomide (TMZ, Cay-14163) in a dose-dependent manner.Formal Name: 4,7-dihydro-6-(1-methylethyl)-7-oxo-5-phenyl-pyrazolo[1,5-a]pyrimidine-3-carbonitrile. CAS Number: 1628208-23-0. Molecular Formula: C16H14N4O. Formula Weight: 278.3. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, DMSO:PBS (pH 7.2) (1:20): 0.05 mg/ml, Ethanol: 5 mg/ml. lambdamax: 239, 280, 322 nm. SMILES: CC(C)C(C(N1C(N2)=C(C#N)C=N1)=O)=C2C3=CC=CC=C3. InChi Code: InChI=1S/C16H14N4O/c1-10(2)13-14(11-6-4-3-5-7-11)19-15-12(8-17)9-18-20(15)16(13)21/h3-7,9-10,19H,1-2H3. InChi Key: DHXKRMSKXLDZGY-UHFFFAOYSA-N.