1. Epigenetics
  2. Histone Methyltransferase
  3. MS023 dihydrochloride

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.

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

CAS No. : 1992047-64-9

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10 mM * 1 mL in DMSO
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Customer Review

Based on 22 publication(s) in Google Scholar

Other Forms of MS023 dihydrochloride:

Top Publications Citing Use of Products

    MS023 dihydrochloride 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 dihydrochloride 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 dihydrochloride 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 dihydrochloride 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 dihydrochloride 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.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    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[1].

    IC50 & Target

    PRMT1

     

    PRMT3

     

    PRMT6

     

    PRMT8

     

    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.

    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±0.2 nM).
    Treatment concentration-dependently reduced the H3R2me2a mark (IC50=56±7 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

    360.32

    Formula

    C17H27Cl2N3O

    CAS No.
    Appearance

    Solid

    Color

    Gray to gray purple

    SMILES

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

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    4°C, stored under nitrogen

    *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 150 mg/mL (416.30 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : 33.33 mg/mL (92.50 mM; Need ultrasonic)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.7753 mL 13.8766 mL 27.7531 mL
    5 mM 0.5551 mL 2.7753 mL 5.5506 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
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    Concentration
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    Volume
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    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

    V1

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    Concentration (final)

    C2

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    In Vivo:

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  PBS

      Solubility: 25 mg/mL (69.38 mM); Clear solution; Need ultrasonic and warming

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
    Purity & Documentation

    Purity: 99.68%

    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    H2O / DMSO 1 mM 2.7753 mL 13.8766 mL 27.7531 mL 69.3828 mL
    5 mM 0.5551 mL 2.7753 mL 5.5506 mL 13.8766 mL
    10 mM 0.2775 mL 1.3877 mL 2.7753 mL 6.9383 mL
    15 mM 0.1850 mL 0.9251 mL 1.8502 mL 4.6255 mL
    20 mM 0.1388 mL 0.6938 mL 1.3877 mL 3.4691 mL
    25 mM 0.1110 mL 0.5551 mL 1.1101 mL 2.7753 mL
    30 mM 0.0925 mL 0.4626 mL 0.9251 mL 2.3128 mL
    40 mM 0.0694 mL 0.3469 mL 0.6938 mL 1.7346 mL
    50 mM 0.0555 mL 0.2775 mL 0.5551 mL 1.3877 mL
    60 mM 0.0463 mL 0.2313 mL 0.4626 mL 1.1564 mL
    80 mM 0.0347 mL 0.1735 mL 0.3469 mL 0.8673 mL
    DMSO 100 mM 0.0278 mL 0.1388 mL 0.2775 mL 0.6938 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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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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    Product Name:
    MS023 dihydrochloride
    Cat. No.:
    HY-19615B
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