CCS-1477 is an inhibitor of p300 and CREB-binding protein (CBP) histone acetyltransferases.1 It selectively binds to p300 and CBP over bromodomain-containing protein 4 (BRD4; Kds = 1.3, 1.7, and 222 nM, respectively). CCS-1477 inhibits the proliferation of OPM-2 multiple myeloma cells (GI50 = 5 nM). It induces tumor regression in MOLM-16 acute myeloid leukemia (AML) and OPM-2 mouse xenograft models when administered at a dose of 20 mg/kg.
1.Brooks, N., Raja, M., Young, B.W., et al.CCS1477: A novel small molecule inhibitor of p300/CBP bromodomain for the treatment of acute myeloid leukaemia and multiple myelomaBlood134(Supplement 1)2560(2019)