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首页-小分子抑制剂&激动剂-Epigenetics-Histone Methyltransferase (HMTase)-MS117
MS117

Chemical Structure : MS117

CAS No.: 2702280-86-0

MS117 (MS-117)

货号: PC-23078Not For Human Use, Lab Use Only.

MS117 is a potent, selective and cell-active covalent PRMT6 inhibitor with Ki of 16 nM and IC50 of 18 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

MS117 is a potent, selective and cell-active covalent PRMT6 inhibitor with Ki of 16 nM and IC50 of 18 nM.
MS117 does not covalently modify other closely related PRMTs and was selective for PRMT6 over other methyltransferases.
MS117 covalently targets a cysteine residue (Cys50) of PRMT6.
MS117 potently and concentration-dependently reduces cellular levels of H3R2 asymmetric dimethylation (H3R2me2a, IC50=1.3 uM) against ectopically expressed PRMT6 in HEK293 cells.
MS117 is not cytotoxic in MCF-7, PNT2, and HEK293T cells.

物理化学性质&存储条件

分子量 298.39
分子式 C17H22N4O
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

N-[3-[4-[[(2-Aminoethyl)methylamino]methyl]-1H-pyrrol-3-yl]phenyl]-2-propenamide

参考文献

1. Shen Y, et al. J Med Chem. 2020 May 28;63(10):5477-5487.

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