Name | CPI-637 |
Synonyms | CPI637 CPI 637 CPI-637 2H-1,5-Benzodiazepin-2-one, 1,3,4,5-tetrahydro-4-methyl-6-[1-methyl-3-(1-methyl-1H-pyrazol-4-yl)-1H-indazol-5-yl]-, (4R)- |
CAS | 1884712-47-3 |
Molecular Formula | C22H22N6O |
Molar Mass | 386.45 |
Density | 1.38±0.1 g/cm3(Predicted) |
Boling Point | 689.2±55.0 °C(Predicted) |
Solubility | DMSO |
pKa | 14.62±0.40(Predicted) |
Storage Condition | -20℃ |
In vitro study | CPI-637 inhibited the expression of MYC in AMO-1 cells (EC50=0.6 μm). |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.588 ml | 12.938 ml | 25.877 ml |
5 mM | 0.518 ml | 2.588 ml | 5.175 ml |
10 mM | 0.259 ml | 1.294 ml | 2.588 ml |
5 mM | 0.052 ml | 0.259 ml | 0.518 ml |
biological activity | CPI-637 is a selective, cytoactive CBP/EP300 bromodomain protein inhibitor. In the TR-FRET assay, the IC50 for CBP and EP300 CPI-637 was 0.03 μm and 0.051 μm, respectively. In other bromine domain, it is highly selective, in contrast, the biochemical activity of BRD9 is more prominent. |
Target | Value |
CBP (Cell-free assay) | 0.03 μM |
EP300 (Cell-free assay) | 0.051 μM |