1. Epigenetics
  2. Histone Methyltransferase
  3. MS023 trihydrochloride

MS023 trihydrochloride 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.

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CAS 番号 : 2108631-19-0

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Top Publications Citing Use of Products

    MS023 trihydrochloride purchased from MedChemExpress. Usage Cited in: Cell Rep Med. 2026 Jan 20;7(1):102542.  [Abstract]

    The drug response curve and IC50 value for PRMT inhibitor MS023 and GSK591 combinations after U2AF2 knockdown in THP1 leukemia cells. Cell viability was assessed using a CCK8 assay.

    MS023 trihydrochloride purchased from MedChemExpress. Usage Cited in: Cell Rep Med. 2026 Jan 20;7(1):102542.  [Abstract]

    RT-PCR results detecting aberrantly spliced transcripts in THP1 leukemia cells, which were treated with PRMT inhibitor MS023 or GSK591 with or without U2AF2 knockdown.

    MS023 trihydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Jan 22;16(1):949.  [Abstract]

    Representative images of FRAP of MSX1-mEGFP- expressing HEK293T treated with DMSO or MS023.

    MS023 trihydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Jan 22;16(1):949.  [Abstract]

    Representative western blot images of Co-IP assays assessing the aDMA of MSX1 in treated with MS023 or PRMT1 siRNA.

    MS023 trihydrochloride purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2025 Mar 8;23(1):126.  [Abstract]

    Immunoprecipitation and western blot analysis of arginine dimethylation in METTL14 overexpressed in HEK293T cells. Cells were treated with 1 μM EPZ015666, 1 μM MS023, or DMSO for 72 h and METTL14 is immunoprecipitated by anti-METTL14 antibody.
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    製品説明

    MS023 trihydrochloride 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[1].

    体外実験

    MS023 (1-1000 nM; 48 hours) inhibits PRMT1 methyltransferase activity in MCF7 cells[1].
    MS023(1-1000 nM; 20 hours) inhibits PRMT6 methyltransferase activity in HEK293 cells[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Western Blot Analysis[1]

    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 nM).Treatment concentration-dependently reduced the H3R2me2a mark (IC50=56 nM).
    体内実験

    Administration of MS023 (160 mg/kg, i.p) in combination with PKC412 (100 mg/kg, i.g.) blocks MLL-r acute lymphoblastic leukemia (ALL) propagation by inhibiting maintenance of functional MLL-r ALL-initiating cells[2].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: NOD-scid IL2Rgnull (NSG) mice bearing primary MLL-r ALL cells[2]
    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.
    分子量

    396.78

    分子式

    C17H28Cl3N3O

    CAS 番号
    SMILES

    CC(OC1=CC=C(C=C1)C2=CNC=C2CN(CCN)C)C.Cl.Cl.Cl

    輸送条件

    Room temperature in continental US; may vary elsewhere.

    保管条件

    Please store the product under the recommended conditions in the Certificate of Analysis.

    純度とドキュメンテーション
    参考文献
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    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    製品名:
    MS023 trihydrochloride
    製品番号:
    HY-19615A
    数量:
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