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首页-小分子抑制剂&激动剂-Epigenetics-Histone Methyltransferase (HMTase)-GSK126
GSK126

Chemical Structure : GSK126

CAS No.: 1346574-57-9

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GSK126 (GSK2816126A, GSK-126)

货号: PC-21939Not For Human Use, Lab Use Only.

GSK126 (GSK2816126A) is a potent, highly selective, and SAM-competitive inhibitor of EZH2 methyltransferase with IC50 of 9.9 nM.

规格 价格 库存 数量
10 mg ￥980 In stock
25 mg ￥1580 In stock
50 mg ￥2480 In stock
100 mg ￥3680 In stock
200 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

GSK126 (GSK2816126A) is a potent, highly selective, and SAM-competitive inhibitor of EZH2 methyltransferase with IC50 of 9.9 nM.
GSK126 potently inhibits both wild-type and mutant EZH2 methyltransferase activity with similar potencies (Kiapp = 0.5-3 nM).
GSK126 is more than 1,000-fold selective for EZH2 versus 20 other human methyltransferases, including both SET-domain-containing and non-SET-domain-containing methyltransferases, 150-fold selective over EZH1.
GSK126 decreases global H3K27me3 levels and reactivates silenced PRC2 target genes. effectively inhibits the proliferation of EZH2 mutant DLBCL cell lines and markedly inhibits the growth of EZH2 mutant DLBCL xenografts in mice.

物理化学性质&存储条件

分子量 526.69
分子式 C31H38N6O2
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-(sec-Butyl)-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3-methyl-6-(6-(piperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxamide

参考文献

1. McCabe MT, et al. Nature. 2012 Dec 6;492(7427):108-12.

2. De Martino M, et al. Cell Cycle. 2023 Dec-Dec;22(23-24):2552-2565.

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