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首页-小分子抑制剂&激动剂-Epigenetics-Histone Methyltransferase (HMTase)-GSK343
GSK343

Chemical Structure : GSK343

CAS No.: 1346704-33-3

GSK343 (GSK 343, GSK-343)

货号: PC-21950Not For Human Use, Lab Use Only.

GSK343 is a highly potent, selective, SAM-competitive, and cell-active EZH2 inhibitor with IC50 of 4 nM and Kiapp of 1.2 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

GSK343 is a highly potent, selective, SAM-competitive, and cell-active EZH2 inhibitor with IC50 of 4 nM and Kiapp of 1.2 nM.
GSK343 displays 60-fold selectivity over EZH1, and >1000-fold over other methyltransferases.
GSK343 potently inhibits H3K27me3 in HCC1806 breast cancer cells with IC50 of 174 nM.

物理化学性质&存储条件

分子量 541.70
分子式 C31H39N7O2
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

1-Isopropyl-N-((6-methyl-2-oxo-4-propyl-1,2-dihydropyridin-3-yl)methyl)-6-(2-(4-methylpiperazin-1-yl)pyridin-4-yl)-1H-indazole-4-carboxamide

参考文献

1. Verma SK, et al. ACS Med Chem Lett. 2012 Oct 19;3(12):1091-6.

2. Amatangelo MD, et al. Cell Cycle. 2013 Jul 1;12(13):2113-9.

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