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GSK126

促销

EZH2 抑制剂

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产品目录号: A11757

库存状态:中国现货中国现货

产品名 目录号 价格 数量
GSK126 2mg A11757-2
¥ 400.00
GSK126 5mg A11757-5
¥ 600.00
GSK126 10mg A11757-10
¥ 900.00
GSK126 25mg A11757-25
¥ 1,600.00

产品仅用于研究,不针对患者销售,望谅解.

产品简介

GSK126 is a potent, highly selective, S-adenosyl-methionine-competitive, small-molecule inhibitor of EZH2 methyltransferase activity, decreases global H3K27me3 levels and reactivates silenced PRC2 target genes.

GSK126

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顾客使用 Adooq 产品发表的高质量科研文献
Adooq 顾客使用 GSK126 发表的文献 (3)
  • Hirosumi Tamura,et al. Evaluation of anticancer agents using patient-derived tumor organoids characteristically similar to source tissues, Oncol Rep, 2018, Aug; 40(2): 635-646 29917168
  • Dupret B,et al. The histone lysine methyltransferase Ezh2 is required for maintenance of the intestine integrity and for caudal fin regeneration in zebrafish, Biochim Biophys Acta Gene Regul Mech, 2017, Oct;1860(10):1079-1093 28887218
  • Theresa Baker,et al. Acquisition of a single EZH2 D1 domain mutation confers acquired resistance to EZH2-targeted inhibitors, Oncotarget, 2015, Oct 20; 6(32): 32646-32655 26360609

Chemical Information

目录号 A11757
Mechanism of action Inhibitor
分子量 526.67
化学分子式 C31H38N6O2
Solubility DMSO
纯度 >98%
储存方式 at -20°C 2 years
CAS No. 1346574-57-9
Synonyms GSK 126, GSK-126
SMILES code CC[C@H](C)N1C=C(C2=C(C=C(C=C21)C3=CN=C(C=C3)N4CCNCC4)C(=O)NCC5=C(C=C(NC5=O)C)C)C
化学名称 (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

生物活性

Description
GSK126 is a potent, highly selective, S-adenosyl-methionine-competitive, small-molecule inhibitor of EZH2 methyltransferase activity, decreases global H3K27me3 levels and reactivates silenced PRC2 target genes.
Targets
EZH2
9.9 nM

制备储备液

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.1 mM 18.99 mL 94.94 mL 189.87mL
0.5 mM 3.8 mL 18.99 mL 37.97 mL
1 mM 1.9 mL 9.49 mL 18.99 mL
5 mM 0.38 mL 1.9 mL 3.8 mL

*The above data is based on the productmolecular weight 526.67. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

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