BET BD2-IN-1_product_DataBase

Bioactivity	BET BD2-IN-1 (compound 45) is a potent and selective inhibitor of BET BD2 (IC50=1.6 nM). BET BD2-IN-1 inhibits the differentiation of Th17 cells by decreasing the activation of STAT3 and NF-κB. BET BD2-IN-1 is used in psoriasis and inflammatory bowel disease (IBD) research[1].
Invitro	BET BD2-IN-1 (500 nM) 能有效抑制 Th17 细胞分化，对 BD2 的选择性优于 BD1[1]。BET BD2-IN-1 (4 nM) 在完整细胞中与 BRD4 BD2 结合，对 BRD4 BD2 具有稳定效应[1]。 0 --> BET BD2-IN-1 相关抗体: Cell Differentiation Assay[1] Cell Line:
In Vivo	BET BD2-IN-1 (20 mg/kg，静脉注射；每日 1 次，连用 7 天) 可抑制小鼠皮肤组织中 p-STAT3 和 p-NF-κB 蛋白的表达，有效改善银屑病小鼠模型的病理改变[1]。BET BD2-IN-1 (20 mg/kg，静脉注射；每日 1 次，连用 7 天) 显著降低 DSS 诱导的 IBD 小鼠模型疾病活动指数 (DAI) 评分[1]。Pharmacokinetic Analysis of BET BD2-IN-1 in Sprague Dawley Rats Model[1] parameter
Name	BET BD2-IN-1
CAS	2677039-24-4
Formula	C30H30N4O2
Molar Mass	478.58
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[1]. Wang Z, et al. Discovery of a Bromodomain and Extra Terminal Domain (BET) Inhibitor with the Selectivity for the Second Bromodomain (BD2) and the Capacity for the Treatment of Inflammatory Diseases. J Med Chem. 2023 Aug 10;66(15):10824-10848.

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