MS023

MS023 is an inhibitor of type I protein arginine methyltransferases (PRMTs; IC₅₀s = 30, 119, 83, 4, and 5 nM for PRMT1, -3, -4, -6, and -8, respectively).¹ It is selective for these type I PRMTs over PRMT5, -7, and -9, as well as a panel of 25 protein lysine methyltransferases (PKMTs) and DNA methyltransferases (DNMTs) when used at a concentration of 10 µM. It inhibits the methylation of histone 4 at arginine 3 (H4R3) in MCF-7 breast cancer cells (IC₅₀ = 9 nM) and H3R2 in HEK293 cells (IC₅₀ = 56 nM). MS023 (20 µM) also inhibits the methylation of the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) nucleocapsid protein and the replication of SARS-CoV-2 in Vero E6 cells.² It reduces tumor growth in a Huh7 mouse xenograft model when administered at a dose of 160 mg/kg.³

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1. Eram, M.S., Shen, Y., Szewczyk, M.M., et al. A potent, selective, and cell-active inhibitor of human type I protein arginine methyltransferases. ACS Chem. Biol. 11(3), 772-781 (2015).

2. Cai, T., Yu, Z., Wang, Z., et al. Arginine methylation of SARS-Cov-2 nucleocapsid protein regulates RNA binding, its ability to suppress stress granule formation, and viral replication. The Journal of Biological Chemisty 297(1), 100821 (2021).

3. Hu, G., Yan, C., Xie, P., et al. PRMT2 accelerates tumorigenesis of hepatocellular carcinoma by activating Bcl2 via histone H3R8 methylation. Exp. Cell Res. 394(2), 112152 (2020).