Overview

  • Product name

    MS023, PRMT inhibitor
  • Description

    Potent, selective, cell-active PRMT inhibitor.
  • Biological description

    MS023 is a potent, selective, and cell-active Type I PRMT inhibitor. IC50 values are 30 nM (PRMT1), 119 nM (PRMT3), 83 nM (PRMT4), 4 nM (PRMT6) and 5 nM (PRMT8). It potently reduces cellular levels of H4R3me2a in MCF7 and HEK293 cells by inhibiting PRMT1/6 methyltransferase activity with IC50 values of 9 nM and 56 nM, respectively. MS023 also inhibits cell growth and potentially induces growth arrest and flattening morphology at low concentrations. It displayed high potency for type I PRMTs including PRMT1, 3, 4, 6 and 8, but displayed no activity against type II and type III PRMTs, protein lysine methyltransferases and DNA methyltransferases. Cellular levels of histone arginine asymmetric dimethylation were potently reduced by MS023. It also reduced global levels of arginine asymmetric dimethylation whilst increasing levels of arginine monomethylation and symmetric dimethylation in cells. MS023 is active in cells.

  • Purity

    > 99%
  • CAS Number

    1831110-54-3
  • Chemical structure

    Chemical Structure

Properties

  • Chemical name

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

  • Molecular weight

    287.40
  • Molecular formula

    C17H25N3O
  • PubChem identifier

    92136227
  • Storage instructions

    Shipped at 4°C. Store at -20°C.
  • Solubility overview

    Soluble in DMSO to 100 mM and in ethanol to 100 mM

  • Handling

    Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.

    Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.

  • SMILES

    CC(C)OC1=CC=C(C=C1)C2=CNC=C2CN(C)CCN
  • Source

    Synthetic

References

This product has been referenced in:

  • Eram MS  et al. A Potent, Selective, and Cell-Active Inhibitor of Human Type I Protein Arginine Methyltransferases. ACS Chem Biol 11:772-781 (2016). Read more (PubMed: 26598975) »
See all 2 Publications for this product

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