1831110-54-3

Basic information

• Product Name: MS023
• Synonyms: MS023;N1-Methyl-N1-[[4-[4-(1-methylethoxy)phenyl]-1H-pyrrol-3-yl]methyl]-1,2-ethanediamine
• CAS NO: 1831110-54-3
• Molecular Formula: C17H25N3O
• Molecular Weight: 287.3999
• Mol File: 1831110-54-3.mol
• Article Data: 0

Chemical Properties

• Boiling Point: 437.8±45.0 °C(Predicted)
• Appearance: /
• Density: 1.075±0.06 g/cm3(Predicted)
• Storage Temp.: -20°C
• Solubility: ≥28.7 mg/mL in DMSO; ≥13.7 mg/mL in EtOH; ≥23.3 mg/mL in H2O
• PKA: 17.44±0.50(Predicted)
• CAS DataBase Reference: MS023(CAS DataBase Reference)
• NIST Chemistry Reference: MS023(1831110-54-3)
• EPA Substance Registry System: MS023(1831110-54-3)

Safety Data

• Hazardous Substances Data: 1831110-54-3(Hazardous Substances Data)

Usage

Description

MS023 is a potent, selective, and cell-active inhibitor of human type PRMTs (protein arginine methyltransferase), which are involved in various biological processes. It is particularly effective against type I PRMTs, including PRMT1, -3, -4, -6, and -8, and has shown potential in reducing cellular levels of histone arginine asymmetric dimethylation. Overexpression of PRMTs is associated with certain cancers, making MS023 a valuable chemical tool for testing biological and therapeutic hypotheses.

Uses

Used in Cancer Research:
MS023 is used as an inhibitor of PRMTs for its potential role in cancer research. It has demonstrated high potency against type I PRMTs, which are related to the development and progression of some cancers. By inhibiting these enzymes, MS023 may help in understanding the underlying mechanisms of cancer and contribute to the development of novel therapeutic strategies.
Used in Drug Development:
MS023 is used as a chemical tool in the development of new drugs targeting PRMTs. Its selectivity and potency against specific PRMTs make it a valuable compound for designing and testing new therapeutic agents that could potentially treat cancer and other diseases associated with PRMT overexpression.
Used in Biological Studies:
MS023 is used as a research tool for studying the role of PRMTs in various biological processes. Its ability to selectively inhibit type I PRMTs allows researchers to investigate the specific functions of these enzymes and their potential involvement in disease pathways.
Used in Pharmaceutical Industry:
MS023 is used as a starting point for the development of new drugs in the pharmaceutical industry. Its potent and selective inhibition of PRMTs makes it a promising candidate for further optimization and development into a therapeutic agent for cancer and other related diseases.

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.

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.