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18nM。
货号:ajcx31116
CAS:N/A
分子式:C17H22N4O
分子量：298.38
溶解度:N/A
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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

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].

[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.