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CPI-637 is a potent and selective CBP/EP300 bromodomains inhibitor with IC50 of 0.03±0.01μM and 11.0±0.6 μM for CBP/EP300 and BRD4, respectively. CPI-637 was also highly selective against other bromodomains (detailed list in the Supporting Information), displaying substantial biochemical activity only against BRD9, which is acceptable, since inhibition of the BRD9 bromodomain has not been shown to produce a pronounced cellular phenotype . In a cellular assay, CPI-637 inhibits the expression of MYC, a transcription factor widely expressed in human cancer,with an EC50 of 0.60 μM, providing an orthogonal measure of the target engagement of the compound.
| Molecular Weight | 386.45 |
| Formula | C22H22N6O |
| CAS Number | 1884712-47-3 |
| Solubility (25°C) | DMSO: ≥ 15 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Epigenetic Reader Domain Products |
|---|
| dBRD9 dihydrochloride
dBRD9 dihydrochloride is a selective BRD9 PROTAC degrader. |
| BBC0403
BBC0403 is a selective BRD2 inhibitor with Kds of 7.64 μM and 41.37 μM for BRD2 (BD2) and BRD2 (BD1), respectively. |
| BAY-155
BAY-155 is a potent and selective menin-MLL tool inhibitor, with an IC50 of 8 nM. |
| FHT-1015
FHT-1015 is a potent SMARCA4/SMARCA2 ATPase (BRG1 and BRM) inhibitor with IC50s of ≤10 nM. |
| ISOX-DUAL
ISOX-DUAL is a dual CBP/BRD4 inhibitor with IC50 values of 0.65 μM and 1.5 μM for CBP and BRD4, respectively. |
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Products are for research use only. Not for human use. We do not sell to patients.
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