MS417 (GTPL-7512) is a highly specific BET bromodomain inhibitor that binds to BRD4-BD1 and BRD4 BD2 with Kd of 36.1 uM and 25.4 uM respectively.
MS417 shows 100-200-fold weaker affinity for CBP, BRD7, or BPTF, and no binding affinity for many other bromodomains.
MS417 blocks BRD4 binding to the acetylated NF-κB, effectively attenuates NF-κB transcriptional activation of proinflammatory genes in kidney cells treated with TNFα or infected by HIV.
MS417 ameliorates inflammation and kidney injury in HIV-1 transgenic mice.
