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MS023 dihydrochloride

CAS No. 1992047-64-9

MS023 dihydrochloride( —— )

Catalog No. M35545 CAS No. 1992047-64-9

MS023 dihydrochloride (MS023 2HCl) is a selective, cytosolic and highly potent inhibitor of human type I protein arginine methyltransferases (PRMTs) with antitumour activity, inhibits PRMT1, PRMT3, PRMT4, PRMT6, and PRMT8.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    MS023 dihydrochloride
  • Note
    Research use only, not for human use.
  • Brief Description
    MS023 dihydrochloride (MS023 2HCl) is a selective, cytosolic and highly potent inhibitor of human type I protein arginine methyltransferases (PRMTs) with antitumour activity, inhibits PRMT1, PRMT3, PRMT4, PRMT6, and PRMT8.
  • Description
    MS023 dihydrochloride is a potent, selective, and cell-active inhibitor of human type I protein arginine methyltransferases (PRMTs) inhibitor, with IC50s of 30, 119, 83, 4 and 5 nM for PRMT1, PRMT3, PRMT4, PRMT6, and PRMT8, respectively.
  • In Vitro
    Western Blot Analysis Cell Line:MCF7 and HEK293 cells Concentration:1.4, 4, 12, 37, 111, 333, and 1000 nM Incubation Time:48 hours for MCF7 cells; 20 hours for HEK293 cells Result:Treatment potently and concentration-dependently reduced cellular levels of H4R3me2a (IC50=9±0.2 nM). Treatment concentration-dependently reduced the H3R2me2a mark (IC50=56±7 nM).
  • In Vivo
    Animal Model:NOD-scid IL2Rgnull (NSG) mice bearing primary MLL-r ALL cells Dosage:160 mg/kg Administration:Intraperitoneal injection; PKC412 (100 mg/kg, i.g.), MS023 (160 mg/kg, i.p), or a combination for 4 weeks Result:Combinatorial treatment extended survival of leukemic mice relative to single treatments.
  • Synonyms
    ——
  • Pathway
    Others
  • Target
    Other Targets
  • Recptor
    Histone Methyltransferase
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    1992047-64-9
  • Formula Weight
    360.32
  • Molecular Formula
    C17H27Cl2N3O
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : ≥ 150 mg/mL (416.30 mM; )H2O : 33.33 mg/mL (92.50 mM; Ultrasonic)
  • SMILES
    Cl.Cl.CC(C)Oc1ccc(cc1)-c1c[nH]cc1CN(C)CCN
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

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.?
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