BET BD2-IN-1 (compound 45) is a potent, selective inhibitor of BET BD2, exhibiting an IC50 value of 1.6 nM. It suppresses Th17 cell differentiation through the reduced activation of STAT3 and NF-κB, making it relevant in research on psoriasis and inflammatory bowel disease (IBD) [1].

BRD2 BD1:570 nM, BRD2 BD2:5.9 nM, BRD3 BD1:465 nM, BRD3 BD2:6.0 mM, BRD4 BD1:524 nM, BRD4 BD2:1.6 nM, BRDT BD1:527 nM

BET BD2-IN-1（500 nM）能有效抑制Th17细胞分化，并且显示出对BD2的高选择性，胜过BD1[1]。而在4 nM浓度下，BET BD2-IN-1在活细胞中稳定结合至BRD4 BD2，表明其对BRD4 BD2具有持久作用[1]。

BET BD2-IN-1（20 mg/kg，静脉注射；每日1次，连续7天）在小鼠皮肤组织中显著抑制p-STAT3和p-NF-κB蛋白的表达，有效缓解银屑病小鼠模型的病理状况[1]。同样条件下，该化合物在DSS诱导的IBD小鼠模型中显著降低疾病活动指数（DAI）评分[1]。对BET BD2-IN-1在Sprague Dawley大鼠模型中进行药动学分析显示，其参数AUC(0‑t)、C0、T1/2、CL和Vdss分别为（单位保留英文原文）[1]。