GSK-340 |CAS:2222509-79-5 Probechem Biochemicals

Chemical Structure : GSK-340

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GSK-340 (GSK340;GSK 340)

货号: PC-63487Not For Human Use, Lab Use Only.

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.

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生物&药学活性

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.
GSK-340 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).
GSK-340 inhibits BRD4 BD2, BRD3 BD2, BRD2 BD2 and BRD4T BD2 with pIC50 of 7.2, 6.5, 7.3 and 6.7, respectively.
GSK-340 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.

物理化学性质&存储条件

分子量	417.553
分子式	C26H31N3O2
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	(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

参考文献

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

GSK-340 (GSK340;GSK 340)

生物&药学活性

物理化学性质&存储条件

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GSK-340 (GSK340;GSK 340)

生物&药学活性

物理化学性质&存储条件

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