GSK040

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

GSK040 

GSK040 是一种有效和具有选择性的 BET BD2 抑制剂，pIC50 值为 8.3。GSK040 对 BET BD2 的选择性比 BET BD1 (pIC50=4.6) 高 5000 倍。GSK040 可用于肿瘤学和免疫学疾病的研究。

GSK040

GSK040 Chemical Structure

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生物活性

GSK040 is a potent and highly selective BET BD2 inhibitor, with a pIC50 of 8.3. GSK040 shows more than 5000-fold selectivity for BET BD2 over BET BD1 (pIC50=4.6). GSK040 can be used for the research of oncology and immunology diseases[1].

IC50 & Target[1]

BD2

8.3 (pIC50)

体内研究
(In Vivo)

GSK040 (1 mg/kg; i.v.) exhibits t1/2 (0.19 h), CLb (50 mL/min/kg) and Vss (0.6 L/kg) in rats[1].
GSK040 (3 mg/kg; p.o.) exhibits oral bioavailability (16%), tmax (0.25 h), Cmax (398 nM) in rats[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

502.60

Formula

C29H34N4O4
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Rianjongdee F, et, al. Discovery of a Highly Selective BET BD2 Inhibitor from a DNA-Encoded Library Technology Screening Hit. J Med Chem. 2021 Jul 12.

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