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首页-小分子抑制剂&激动剂-Epigenetics-Histone Methyltransferase (HMTase)-EPZ005687
EPZ005687

Chemical Structure : EPZ005687

CAS No.: 1396772-26-1

EPZ005687 (EPZ 005687)

货号: PC-21951Not For Human Use, Lab Use Only.

EPZ005687 is a potent, selective and SAM-competitive inhibitor of EZH2 with Ki of 24 nM, 50-fold selectivity over EZH1 and 500-fold selectivity against 15 other protein methyltransferases.

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10 mg ¥880 In stock
25 mg ¥1380 In stock
50 mg ¥2180 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

EPZ005687 is a potent, selective and SAM-competitive inhibitor of EZH2 with Ki of 24 nM, 50-fold selectivity over EZH1 and 500-fold selectivity against 15 other protein methyltransferases.
EPZ005687 reduces H3K27 methylation in various lymphoma cells.
EPZ005687 suppresses cell proliferation and migration in sarcoma cell lines.

物理化学性质&存储条件

分子量 539.68
分子式 C32H37N5O3
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-Cyclopentyl-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-6-(4-(morpholinomethyl)phenyl)-1H-indazole-4-carboxamide

参考文献

1. Knutson SK, et al. Nat Chem Biol. 2012 Nov;8(11):890-6.

2. Shen JK, et al. Sci Rep. 2016 Apr 29;6:25239.

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