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.
