MS049

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)