GSK-340 ( GSK340;GSK 340 )

产品货号. M13548 CAS No. 2222509-79-5

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Datasheet

HNMR

HPLC

MSDS

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产品名称

GSK-340
注意事项

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断
产品简述

GSK-340 is a potent, selective inhibitor of second bromodomains of the BET family (BD2).
产品描述

GSK-340 is a potent, selective inhibitor of second bromodomains of the BET family (BD2) with pKd of 8.18, 7.49, 7.72 and 7.68 for BRD4 BD2, BRD3 BD2, BRD2 BD2 and BRD4T BD2, respectively; displays 229-, 40-, 48- and 91-fold selectivity over the responding BD1, >100-fold selectivity over TAF1, WRD9, ATAD2A/B and other bromodomains (pKd<5.0); inhibits BRD4 BD2, BRD3 BD2, BRD2 BD2 and BRD4T BD2 with pIC50 of 7.2, 6.5, 7.3 and 6.7, respectively; inhibits release of the MCP-1 cytokine in human PBMCs (pIC50=7.4) and whole blood; GSK-340 is an useful in vitro tool molecule for investigation into the biological role of the BD2 domains.
同义词

GSK340;GSK 340
通路

Chromatin/Epigenetic
靶点

Bromodomain
受体

Bromodomain
研究领域

——
适应症

——

CAS Number

2222509-79-5
分子量

417.55
分子式

C26H31N3O2
纯度

>98% (HPLC)
溶解度

——
SMILES

——
化学全称

(S)-1-(2-cyclopropyl-4-(2-(hydroxymethyl)benzyl)-6-(1,2,3,6-tetrahydropyridin-4-yl)-3,4-dihydroquinoxalin-1(2H)-yl)ethan-1-one

1. Law RP, et al. J Med Chem. 2018 May 3. doi: 10.1021/acs.jmedchem.7b01666.

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