NHWD-870 is a potent BET inhibitor with IC50 of 2.7 nM for BRD4 bromodomain, inhibits BRD4 activation and c-MYC expression.
NHWD-870 shows potent BET inhibition in cellular assays using A375 melanoma cells with IC50 of 2.46 nM, which is about 23-fold more potent than I-BET151 (IC50 = 55.5 nM), and about 14-fold more potent than two clinical stage inhibitors GSK-525762 (IC50 = 35.6 nM) or OTX015 (IC50=34.8 nM).
NHWD-870 suppresses the growth of multiple solid tumor cell lines, inhibits BRD4 phosphorylation and c-MYC expression.
NHWD-870 strongly suppresses the growth of established lung tumor, ovarian tumor, lymphoma, and melanoma in vivo.
NHWD-870 reduced the proliferation of TAMs in vivo, by inhibiting CSF1R signaling.
