ms023

MS023 is a potent, selective, and cell-active Type I PRMT inhibitor with IC50 values of 30 nM, 119 nM, 83 nM, 4 nM, and 5 nM for PRMT1, PRMT3, PRMT4, PRMT6, and PRMT8, respectively.

MS023 trihydrochloride (MS023 3HCl) is a selective and potent human type I protein arginine methyltransferase (PRMT) inhibitor with potential anticancer activity against PRMT1, PRMT3, PRMT4, PRMT6, and PRMT8 for cancer research.

MS023 dihydrochloride (MS023 2HCl) is a selective, cytosolic and highly potent inhibitor of human type I protein arginine methyltransferases (PRMTs) with antitumour activity, inhibits PRMT1, PRMT3, PRMT4, PRMT6, and PRMT8, and increases the proliferative capacity of isolated cultured MuSC. It can be used to study breast cancer.

C-MS023 is a photoactivatable prodrug of MS023, designed to achieve spatiotemporal inhibition of Histone Arginine Asymmetric Dimethylation. It specifically inhibits PRMT6-mediated asymmetric dimethylation of H3 Arginine 2 (H3R2me2a) with an IC50 of approximately 0.2224 μM. The photolysis of C-MS023 can be triggered by exposure to 420 nm visible light, releasing MS023, which effectively downregulates histone arginine asymmetric dimethylation and transcriptional activities related to DNA replication.

MS023 is a type I PRMT inhibitor (IC50: 20, 119, 83, 8, and 8 nM for PRMT1, 3, 4, 6, and 8, respectively).