MS023

Description

MS023 is a potent, selective, and cell-active inhibitor of human type PRMTs (protein arginine methyltransferase), which is involved in many biological processes. Overexpression of PRMTs is related to some cancers. Therefore, MS023 is a useful chemical tools for testing biological and therapeutic hypotheses. MS023 displayed high potency for type I PRMTs including PRMT1, -3, -4, -6, and -8 but was completely inactive against type II and type III PRMTs, protein lysine methyltransferases and DNA methyltransferases. MS023 potently decreased cellular levels of histone arginine asymmetric dimethylation. It also reduced global levels of arginine asymmetric dimethylation and concurrently increased levels of arginine monomethylation and symmetric dimethylation in cells.

References

https://www.caymanchem.com/product/18361
Eram, Mohammad S., et al. "A Potent, Selective, and Cell-Active Inhibitor of Human Type I Protein Arginine Methyltransferases." Acs Chemical Biology 11.3(2015):772-781.

Uses

MS023 is a potent inihbitor of PRMTs 1,3,4,6,and 8 (IC50 = 30, 119, 83, 8, and 8 nM, respectively), which are responsible for asymmetric dimethylation of arginine residues.

Biological Activity

ms023 is a type i prmts inhibitor.protein arginine methyltransferases (prmts) play a critical role in various biological processes. prmt overexpression has been observed in a variety of human diseases including cancer. prmts has been divided into three categories: type i prmts for catalyzing mono- and asymmetric dimethylation of arginine residues, type ii prmts for catalyzing mono- and symmetric dimethylation of arginine residues, and type iii prmt for catalyzing only monomethylation of arginine residues.

Biochem/physiol Actions

MS023 is a potent and selective chemical probe for Type I protein arginine methyltransferases (PRMTs). MS023 is a potent inihbitor of PRMTs 1,3,4,6,and 8 (IC50 = 30, 119, 83, 8, and 8 nM, respectively), which are responsible for asymmetric dimethylation of arginine residues. MS023 is active in cells. For full characterization details, please visit the MS023 probe summary on the Structural Genomics Consortium (SGC) website.To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc

in vitro

previous study showed that ms023 had excellent potency for type i prmts but was completely inactive to both type ii and type iii prmts, protein lysine methyltransferases as well as dna methyltransferases. moreover, the crystal structure of prmt6 with ms023 indicated that ms023 bound to the substrate binding site. in addition, ms023 could potently decrease the cellular levels of histone arginine asymmetric dimethylation. furthermore, ms023 could reduce the levels of arginine asymmetric dimethylation and could also concurrently increase the cellular levels of both arginine monomethylation and symmetric dimethylation [1].

IC 50

30, 119, 83, 4, and 5 nm for prmt1, prmt3, prmt4, prmt6 and prmt8, respectively.

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.