Molibresib

BET proteins:35 nM

在分化的第2天,I-BET-762处理可改变CD4+T细胞的细胞因子产生,使一些抗炎基因产物的表达上调,并使一些促炎细胞因子的表达下调。I-BET-762抑制溴区和额外的末端结构域的蛋白和BRD2/3/4结合到BET的串联溴区（Kd：50.5-61.3 nM）, 在FRET分析中,置换BET串联溴区一种四乙酰化的H4肽（IC50：32.5-42.5 nM）。

连续两天每日注射两次I-BET-762,可使小鼠免于脓毒症造成的死亡.I-BET-762可防止细菌诱导的脓毒病和脂多糖诱导的内毒素休克.脂多糖注射后1.5 h,I-BET-762可治愈小鼠.在实验性自身免疫性脑脊髓炎小鼠模型中,I-BET-762早期处理可抑制Th1分化的2D2 T细胞诱发神经性炎症的能力.

H2O:<1 mg/mL,DMSO:78 mg/mL (184 mM),Ethanol:39 mg/mL (92 mM)

CD4+ T cells are isolated from lymph nodes and spleens of 10- to 12-wk old mice and activated with plate bound anti-CD3 and anti-CD28 antibodies in the presence of indicated cytokines. I-BET-762 compounds is included during the 60–72 h of initial activation. Over the course of 5 d of T-cell culture and expansion, the compounds is diluted 12-fold relative to the starting concentrations.(Only for Reference)