MS117

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

MS117  纯度: ≥98.0%

MS117 是首创的、具有细胞活性的、不可逆的蛋白精氨酸甲基转移酶 (PRMT6) 的共价抑制剂,其 IC50 值为18 nM。

MS117

MS117 Chemical Structure

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生物活性

MS117 is a first-in-class and cell-active irreversible protein arginine methyltransferase 6 (PRMT6) covalent inhibitor, with an IC50 of 18 nM[1].

IC50 & Target

IC50: 18 nM (PRMT6), 100 nM (PRMT1), 110 nM (PRMT8), 3 μM (PRMT3), 4 μM (PRMT4)[1].

体外研究
(In Vitro)

MS117 (Compound 4) inhibits the PRMT6 methyltransferase activity in a time-dependent manner[1].
MS117 (Compound 4) shows moderate selectivity (6-fold) for PRMT6 over PRMT1 (IC50 = 0.1 ± 0.025 µM) and PRMT8 (IC50 = 0.11 ± 0.01 µM) [1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

298.38

Formula

C17H22N4O

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
参考文献
  • [1]. Yudao Shen, et al. Discovery of a First-in-Class Protein Arginine Methyltransferase 6 (PRMT6) Covalent Inhibitor. J Med Chem. 2020 May 28;63(10):5477-5487.

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