Potent and selective BRD4 bromodomain inhibitor (Ki
= 30 - 50 nM for the first bromodomain (BRD4(1)). Exhibits 10-fold selectivity for BRD4(1) over BRD4(2). Blocks BRD4 transcriptional activity in lipopolysaccharide-induced production of both nitric oxide and IL-6 in mouse macrophages (IC50
values are 3.8 and 4.9 μ
M, respectively). Attenuates melanoma cell proliferation in vitro
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Structure-guided design of potent diazobenzene inhibitors for the BET bromodomains.
Zhang et al.
BRD4 sustains melanoma proliferation and represents a new target for epigenetic therapy.
Segura et al.
Cancer Res., 2013;73:6264