compound introduction
MS117 is a first-in-class and cell-active irreversible protein arginine methyltransferase 6 (PRMT6) covalent inhibitor, with an IC 50 of 18 nM. IC50& Target:IC50: 18 nM (PRMT6), 100 nM (PRMT1), 110 nM (PRMT8), 3 μM (PRMT3), 4 μM (PRMT4) . In Vitro:MS117 (Compound 4) inhibits the PRMT6 methyltransferase activity in a time-dependent manner. MS117 (Compound 4) shows moderate selectivity (6-fold) for PRMT6 over PRMT1 (IC 50 = 0.1 ± 0.025 µM) and PRMT8 (IC 50 = 0.11 ± 0.01 µM). MCE has not ind Biological Activity:MS117 is a first-in-class and cell-active irreversible protein arginine methyltransferase 6 (PRMT6) covalent inhibitor, with an IC 50 of 18 nM.
