CPI-637

CPI-637 is an inhibitor of cyclic-AMP response element binding protein (CBP) and adenoviral E1A binding protein of 300 kDa (EP300), a homologous pair of bromodomain-containing proteins (IC50s = 30 and 51 nM in a time-resolved-FRET (TR-FRET) assay). It is selective for CBP and EP300 over the BET family of bromodomains (IC50s = >10 µM), however, CPI-637 is active at bromodomain BRD9 (IC50 = 0.73 µM). CPI-637 also inhibits MYC expression (EC50 = 0.6 µM) in AMO-1 cells.Formal Name: (4R)-1,3,4,5-tetrahydro-4-methyl-6-[1-methyl-3-(1-methyl-1H-pyrazol-4-yl)-1H-indazol-5-yl]-2H-1,5-benzodiazepin-2-one. CAS Number: 1884712-47-3. Molecular Formula: C22H22N6O. Formula Weight: 386.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: :, DMF: 0.2 mg/ml, DMSO: 0.5 mg/ml, DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml, Ethanol: 0.1 mg/ml. lambdamax: 201, 229, 320 nm. SMILES: CN1N=C(C2=CN(C)N=C2)C3=C1C=CC(C4=C(N[C@H](C)CC(N5)=O)C5=CC=C4)=C3. InChi Code: InChI=1S/C22H22N6O/c1-13-9-20(29)25-18-6-4-5-16(22(18)24-13)14-7-8-19-17(10-14)21(26-28(19)3)15-11-23-27(2)12-15/h4-8,10-13,24H,9H2,1-3H3,(H,25,29)/t13-/m1/s1. InChi Key: BFTKDWYIRJGJCA-CYBMUJFWSA-N.