2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Biological activity
Description
Target:
IC50 value: 4-119 nM
Target: type I PRMTs
In Vivo
In Vitro
MS023 potently inhibits PRMT1 (IC50 = 30 ± 9 nM), PRMT3 (IC50 = 119 ± 14 nM), PRMT4 (IC50 = 83 ± 10 nM), PRMT6 (IC50 = 4 ± 0.5 nM), and PRMT8 (IC50 = 5 ± 0.1 nM). Importantly, MS023 does not inhibit any type II PRMTs (PRMT5 and 9) and type III PRMT (PRMT7) at concentrations up to 10 μM. MS023 displays high potency for type I PRMTs including PRMT1, -3, -4, -6, and -8 but is completely inactive against type II and type III PRMTs, protein lysine methyltransferases and DNA methyltransferases. MS023 potently decreases cellular levels of histone arginine asymmetric dimethylation. It also reduces global levels of arginine asymmetric dimethylation and concurrently increased levels of arginine monomethylation and symmetric dimethylation in cells. [1]
Kinase Assay
Cell Assay
Animal Administration
References
[1]. Eram MS, et al. A Potent, Selective, and Cell-Active Inhibitor of Human Type I Protein Arginine Methyltransferases. ACS Chem Biol. 2016 Mar 18;11(3):772-81.
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