cbp/p300 in 3

CBP/p300-IN-3 (P300/CBP-IN-3) is an inhibitor of p300/CBP histone acetyltransferase.

CBP/p300 ligand 3, a specific target protein ligand of CBPD-268, modulates the function of CBP and p300. These two proteins, which possess histone acetyltransferase (HAT) activity, are crucial in the regulation of gene expression, cell proliferation, differentiation, and DNA repair by acetylating histones and other proteins. This ligand operates by binding to a particular domain within the CBP/p300 proteins (the bromine domain or HAT domain), either inhibiting their enzymatic activity or altering their interactions with other proteins (transcription factors). CBP/p300 ligand 3 is applicable in research on cancer, neurodegenerative diseases, and other conditions marked by abnormal CBP/p300 activity.

CBP/p300-IN-15 (compound 13a) is a potent inhibitor of p300 (IC50: 2.5 nM) and CBP (IC50: 28.0 nM). It inhibits OVCAR-3 cells (EC50: 0.865 μM) and A2780 cells (EC50: 2.71 μM). CBP/p300-IN-15 can be used to study ovarian cancer.