I-CBP112 is a specific and potent inhibitor of CBP/p300 bromodomain with Kd of 150-170 nM.
I-CBP112 displaces H3K56ac from the CBP binding site with an IC50 of 170 nM.
I-CBP112 demonstrates 37-fold and 132-fold selectivity over BRD4 BD1 and BRD4 BD2, respectively.
I-CBP112 increases the cytotoxic activity of JQ1 in leukemic cells.
I-CBP112 impaires the disease-initiating self-renewal leukemic cells in vitro and in vivo without causing significant cytotoxicity.
