A selective, dual PRMT4/PRMT6 inhibitor
MS049 is a potent and selective inhibitor of PRMT4 (IC50 = 34 nM) and PRMT6 (IC50 = 43 nM).1 It is less active against additional type I PRMTs (IC50s = >130, >220, and 1.6 ?M for PRMT1, PRMT3, and PRMT8, respectively) and displays no inhibition against type II or type III PRMTs nor any additional methyltransferases or nonepigenetic targets tested.1 MS049 has been shown to reduce the H3R2me2a mark in HEK293 cells with an IC50 value of 0.97 ?M and also, unexpectedly, to reduce H4R3me2a in HEK293 cells.1 For more information on MS049 please visit the Structural Genomics Consortium (SGC). The negative control, MS049N, for MS049 is also available exclusively through the SGC. You can submit a request to receive the negative control here.
1.Shen, Y., Szewczyk, M.M., Eram, M.S., et al.Discovery of a potent, selective, and cell-active dual inhibitor of protein arginine methyltransferase 4 and protein arginine methyltransferase 6J. Med. Chem.(2016)
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