cbp/p300-in-2

CBP/EP300-IN-2 is an inhibitor of CBP/EP300 with IC50 values of 1.07 nM for CBP/HTRF and 5.96 nM for Myc.

CBP/p300-IN-22 is a selective inhibitor of the CBP/EP300 bromodomain, with an IC50 of 4 nM. It exhibits high selectivity for BRD4(1) and reduces cytokine expression induced by TNF-α as well as subsequent immune cell recruitment by inhibiting NF-κB signaling, demonstrating anticancer properties. This compound is applicable for research into rheumatoid arthritis (RA) and other TNF-α-mediated inflammatory diseases.

CBP/p300-IN-21 (Compound 5d) is a selective inhibitor of CBP/p300, with IC50 values of 0.07 μM for p300 and 1.755 μM for CBP; it reduces H3K18Ac levels and inhibits the growth of 4T1 tumors in mice [1].

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.