cbp/p300 in 2

Thalidomide-NH-CBP/p300 ligand 2 (P-007) is a PROTAC-based compound engineered to degrade the proteins CBP and p300, functioning as a molecular antagonist (WO2020173440).

CBP/p300 ligand 2 is the target protein ligand for PROTAC dCBP-1, a potent and selective p300/CBP degrader.

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].