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MS023, PRMT inhibitor (ab223596)

Key features and details

  • Potent, selective, cell-active PRMT inhibitor.
  • CAS Number: 1831110-54-3
  • Purity: > 99%

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

  • Form / State: Solid
  • Source: Synthetic

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

Images

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