MS023 is a potent and selective chemical probe for Type I PRMTs with IC50 values of 30, 119, 83, 8, and 8 nM for PRMTs 1,3,4,6,and 8, respectively. MS023 is active in cells.
MS023 is a potent, selective, and cell-active inhibitor of human type I PRMTs with IC50 values of 30, 119, 83, 4 and 5nM for PRMT1, 3, 4, 6 and 8, respectively. MS023 inhibited both PRMT1 methyltransferase activity shown by decreased level of H4R3me2a post 48h in MCF7 cells, and PRMT6 methyltransferase activity shown by decreased level of H4R3me2a post 20h in HEK293 cells at concentration>37nM. Treatment with MS023 at 10μM or 50μM for 2 days led a significant decrease in global levels of arginine asymmetric dimethylation (Rme2a) and a concurrent increase in global levels of arginine monomethylation (Rme1) and arginine symmetric demethylation in MCF7 and HEK293 cells[2].
作用机制
MS023 can effectively occupy the arginine side chain binding pocket of the substrate and likely form the substrate-inhibitor-PRMT6 complex without significant penalty of free energy.[2]
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