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首页-小分子抑制剂&激动剂-Epigenetics-Bromodomain-GSK785
GSK785

Chemical Structure : GSK785

CAS No.: 3053860-48-0

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GSK785 (GSK-785)

货号: PC-26244Not For Human Use, Lab Use Only.

GSK785 (GSK-785) is a BRD2/4-selective bivalent BET I nhibitor with pIC50 of 7.9 and 8.5 in PPI assays against the CRDA parameters, shows pIC50 of 7.4 in the hWB MCP1 assay, 125-fold selectivity for BRD2 over BRD3, 13-fold selectivity for BRD2 over BRD4, and 10-fold selectivity for BRD4 over BRD3.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

GSK785 (GSK-785) is a BRD2/4-selective bivalent BET inhibitor with pIC50 of 7.9 and 8.5 in PPI assays against the CRDA parameters, shows pIC50 of 7.4 in the hWB MCP1 assay, 125-fold selectivity for BRD2 over BRD3, 13-fold selectivity for BRD2 over BRD4, and 10-fold selectivity for BRD4 over BRD3.

物理化学性质&存储条件

分子量 538.69
分子式 C33H38N4O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

(R)-7-(7-(((R)-1,3-Dimethyl-2-oxo-2,3-dihydro-1H-benzo[d]azepin-7-yl)methyl)-2,7-diazaspiro[3.5]nonane-2-carbonyl)-1,3-dimethyl-1,3-dihydro-2H-benzo[d]azepin-2-one

参考文献

1. Rianjongdee F, et al. J Med Chem. 2026 Jan 22;69(2):895-917.

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