MS417 是一种 BET 特异性 BRD4 抑制剂，与 BRD4-BD1 和 BRD4-BD2 结合，Kd值分别为 36.1和25.4 nM，IC50值分别为 30和46 nM。它对 CBP BRD 的选择性较低，IC50值为 32.7 μM。

MS417 is an inhibitor of BET-specific BRD4(BRD4-BD1 and BRD4-BD2 with IC50s of 30, 46 nM and Kds of 36.1, 25.4 nM, respectively), with weak selectivity at CBP BRD with IC50 of 32.7 μM.

BET (Bromodomain and Extra-Terminal domain)-specific bromodomain inhibitor MS417, designed to block 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, an animal model for HIVAN[1].

916489-36-6

C20H19ClN4O2S

414.91

GTPL7512

Ethanol:50 mg/mL (120.51 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years