GSK046 是一种选择性和具有口服活性的BET蛋白BD2溴结构域的抑制剂，对BRD2 BD2、BRD3 BD2、BRD4 BD2 和 BRDT BD2的IC50值为 264、98、49 和 214 nM，具有免疫调节活性。

GSK046 is a potent, selective and orally active BD2 bromodomain inhibitor of the BET proteins(IC50s of 264 nM (BRD2 BD2), 98 nM (BRD3 BD2), 49 nM (BRD4 BD2) and 214 nM (BRDT BD2), respectively). It has immunomodulatory activity.

GSK046 (40 mg/kg/QD;?s.c. for 14 days) has immunomodulatory activity.?GSK046 exhibits Cmax (C57BL6 1589, C57B16 2993 ng/mL) and terminal elimination half-lives (C57BL6 1.8, C57B16 1.9 h) following oral administration (C57BL6 10, C57B16 40 mg/kg).?GSK046 exhibits Cmax (mouse 1589, rat 202 ng/mL) and terminal elimination half-lives (mouse 1.8, rat 1.4 h) following oral administration (mouse 10, rat 10 mg/kg)[1].

2474876-09-8

C23H27FN2O4

414.477

iBET-BD2

DMSO:83.33 mg/mL (201.05 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years