2. Epigenetics
  3. Histone Methyltransferase
  4. 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.

For research use only. We do not sell to patients.

CAS No. : 2108631-19-0

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MS023 trihydrochloride Related Antibodies

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.

    View All Histone Methyltransferase Isoform Specific Products:

    View All Isoforms
    EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D ASH1L/KMT2H SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 NSD3/WHSC1L1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

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    Description

    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].

    In Vitro

    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.

    MS023 trihydrochloride Related Antibodies

    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).
    In Vivo

    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.
    Molecular Weight

    396.78

    Formula

    C17H28Cl3N3O
    CAS No.
    SMILES

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

    Room temperature in continental US; may vary elsewhere.
    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.
    Purity & Documentation
    References
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    MS023 trihydrochloride Related Classifications

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    Help & FAQs
    • 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.

    Keywords:

    MS023 trihydrochloride2108631-19-0Histone MethyltransferaseInhibitorinhibitorinhibit

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