cbp brd

MS417 (GTPL7512) is an inhibitor of BET-specific BRD4(BRD4-BD1 and BRD4-BD2 with IC50s of 30, 46 nM and Kds of 36.1, 25.4 nM, respectively), with weak selectivity at CBP BRD with IC50 of 32.7 μM.

Pocenbrodib (FT-7051) is a potent inhibitor of the bromodomain of the CBP/p300 family with potential antitumour activity and is palatable for cancer research.

L-45 is the first potent and cell-active bromodomain (Brd) inhibitor of p300/CBP-associated factor (PCAF) (Kd: 126±15 nM).

CZL-077 is a potent, highly selective, and orally active p300/CBP bromodomain (BRD) inhibitor, with p300 IC50 at 0.034 μM and CBP IC50 at 0.052 μM, demonstrating strong selectivity for the BRD of BET proteins (BRD2/3/4). This compound effectively inhibits the growth of OPM-2 and 22RV1 cells, with IC50 values of 0.024 μM and 5.6 μM, respectively. In xenograft mouse models of OPM-2 and 22RV1, CZL-077 exhibits anti-tumor activity. CZL-077 is applicable for research in multiple myeloma and prostate cancer.

L-Moses (L-45) dihydrochloride is the first potent and selective inhibitor of the p300/CBP-associated factor (PCAF) bromodomain (Brd) with a dissociation constant (Kd) of 126 nM.

SGC-CBP30 is an effective CREBBP/EP300 inhibitor (IC50: 21/38 nM).