An inhibitor of the BRPF1 bromodomain
NI-42 is an inhibitor of the bromodomain and PHD finger-containing 1 (BRPF1) bromodomain (IC50 = 7.9 nM).1 It is selective for BRPF1 over BRPF2/BRD1, BRPF3, BRD9, and BRD4/BD1 (IC50s = 48, 260, 310, and 4,500 nM, respectively).2 NI-42 inhibits the growth of OCI-AML2, Nomo-1, THP-1, KG-1, and MV-4-11 acute myeloid leukemia (AML) cells (GI50s = 1.3, 4.6, 5.7, 7, and 9.9 ?M, respectively) and a variety of non-AML cells (GI50s = 1-10 ?M).1 It also inhibits the growth of DMS114 lung, HRA-19 colon, and RERF-LC-Sq1 lung cancer cells (GI50s = 16.6, 15.6, and 17.1 ?M, respectively) but not NCI H1703 lung cancer cells (GI50 = >30 ?M).2
1.Igoe, N., Bayle, E.D., Fedorov, O., et al.Design of a biased potent small molecule inhibitor of the bromodomain and PHD finger-containing (BRPF) proteins suitable for cellular and in vivo studiesJ. Med. Chem.60(2)668-680(2017) 2.Igoe, N., Bayle, E.D., Tallant, C., et al.Design of a chemical probe for the bromodomain and plant homeodomain finger-containing (BRPF) family of proteinsJ. Med. Chem.60(16)6998-7011(2017)
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