For research use only. Not for therapeutic Use.
CPI-637 is a selective and potent CBP/EP300 bromodomain inhibitor with IC50 values of 0.03 μM, 0.051 μM and 11.0 μM for CBP, EP300 and BRD4 BD-1, respectively, and an EC50 of 0.3 μM for CBP[1].
CPI-637 (Compound 28) inhibits MYC expression in AMO-1 cells (EC50 value of 0.60 μM) [1].
| Catalog Number | I002432 |
| CAS Number | 1884712-47-3 |
| Synonyms | (4R)-4-methyl-6-[1-methyl-3-(1-methylpyrazol-4-yl)indazol-5-yl]-1,3,4,5-tetrahydro-1,5-benzodiazepin-2-one |
| Molecular Formula | C22H22N6O |
| Purity | ≥95% |
| InChI | 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 |
| InChIKey | BFTKDWYIRJGJCA-CYBMUJFWSA-N |
| SMILES | CC1CC(=O)NC2=CC=CC(=C2N1)C3=CC4=C(C=C3)N(N=C4C5=CN(N=C5)C)C |
| Reference | [1]. Taylor AM, et al. Fragment-Based Discovery of a Selective and Cell-Active Benzodiazepinone CBP/EP300 Bromodomain Inhibitor (CPI-637). ACS Med Chem Lett. 2016 Mar 15;7(5):531-6. |
