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.

p300/CBP:4 nM

CBP/p300-IN-22 (Compound 2) at a concentration of 1 μM for 1 hour reduces the expression of cytokines IL-1β, IL-8, MCP-1, and TNF-α in TNF-α-induced THP-1 cells. Additionally, CBP/p300-IN-22 strongly inhibits the growth of leukemia, melanoma, and breast cancer cell lines in an NCI-60 antiproliferative screening over a 0-8 hour period. When used at concentrations of 0.1-10 μM for 3 days, it may reduce the proliferation of THP-1 cells by decreasing MYC expression without affecting normal cells.

CBP/p300-IN-22 (160 μM; subcutaneous and intraperitoneal injections; 90 minutes post rmTNF-α administration) reduced inflammation in a novel mouse model induced by TNF-α.