MS023

Modify Date: 2024-01-09 09:34:48

MS023 Structure
MS023 structure
Common Name MS023
CAS Number 1831110-54-3 Molecular Weight 287.400
Density 1.1±0.1 g/cm3 Boiling Point 437.8±45.0 °C at 760 mmHg
Molecular Formula C17H25N3O Melting Point N/A
MSDS N/A Flash Point 218.6±28.7 °C

 Use of MS023


MS023 is a potent, selective, and cell-active inhibitor of human type I PRMTs with IC50 of 4-119 nM.IC50 value: 4-119 nMTarget: type I PRMTs 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]

 Names

Name N1-Methyl-N1-[[4-[4-(1-methylethoxy)phenyl]-1H-pyrrol-3-yl]methyl]-1,2-ethanediamine
Synonym More Synonyms

 MS023 Biological Activity

Description MS023 is a potent, selective, and cell-active inhibitor of human type I PRMTs with IC50 of 4-119 nM.IC50 value: 4-119 nMTarget: type I PRMTs 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]
Related Catalog
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.

 Chemical & Physical Properties

Density 1.1±0.1 g/cm3
Boiling Point 437.8±45.0 °C at 760 mmHg
Molecular Formula C17H25N3O
Molecular Weight 287.400
Flash Point 218.6±28.7 °C
Exact Mass 287.199768
LogP 2.28
Vapour Pressure 0.0±1.1 mmHg at 25°C
Index of Refraction 1.567
Storage condition -20℃

 Synonyms

N-{[4-(4-Isopropoxyphenyl)-1H-pyrrol-3-yl]methyl}-N-methyl-1,2-ethanediamine
1,2-Ethanediamine, N-methyl-N-[[4-[4-(1-methylethoxy)phenyl]-1H-pyrrol-3-yl]methyl]-
MS023