NI-42

BRPF1溴结构域抑制剂(IC50=7.9nM)；对BRPF1具有选择性，优于BRPF2/BRD1、BRPF3、BRD9和BRD4/BD1（IC50s分别为48、260、310和4,500nM）；抑制OCI-AML2、Nomo-1、THP-1、KG-1和MV-4-11AML细胞（GI50s分别为1.3、4.6、5.7、7和9.9µM）以及多种非AML细胞（GI50s=1-10µM）；还抑制DMS114肺癌、HRA-19结肠癌和RERF-LC-Sq1肺癌细胞（GI50s分别为16.6、15.6和17.1µM）的生长。An inhibitor of the BRPF1 bromodomain (IC50 = 7.9 nM); selective for BRPF1 over BRPF2/BRD1, BRPF3, BRD9, and BRD4/BD1 (IC50s = 48, 260, 310, and 4,500 nM, respectively); inhibits the growth of OCI-AML2, Nomo-1, THP-1, KG-1, and MV-4-11 AML cells (GI50s = 1.3, 4.6, 5.7, 7, and 9.9 µM, respectively) and a variety of non-AML cells (GI50s = 1-10 µM); 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 µM, respectively).