2. Epigenetics
  3. Histone Methyltransferase
  4. MS023

MS023, a chemical probe, 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 : 1831110-54-3

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10 mM * 1 mL in DMSO
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カスタマーレビュー

Based on 22 publication(s) in Google Scholar

Other Forms of MS023:

MS023 関連抗体

Top Publications Citing Use of Products

    MS023 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 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 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 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 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.

    Histone Methyltransferase アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    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

    • 生物活性

    • 純度とドキュメンテーション

    • 参考文献

    • カスタマーレビュー

    製品説明

    MS023, a chemical probe, 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

     

    Cellular Effect
    Cell Line Type Value Description References
    A549 IC50
    13.4 μM
    Compound: Chemical probe: MS023
    Antiproliferative against human A549 cells expressing MTAP clone 2 assessed as reduction of cell death treated for 7 days with replenishment of medium for every 48 hrs by MTT assay (Rvb = 4.4 uM)
    Antiproliferative against human A549 cells expressing MTAP clone 2 assessed as reduction of cell death treated for 7 days with replenishment of medium for every 48 hrs by MTT assay (Rvb = 4.4 uM)
    		[PMID: 33691794]
    A549 IC50
    5.1 μM
    Compound: Chemical probe: MS023
    Antiproliferative against human A549 cells expressing MTAP clone 1 assessed as reduction of cell death treated for 7 days with replenishment of medium for every 48 hrs by MTT assay (Rvb = 4.4 uM)
    Antiproliferative against human A549 cells expressing MTAP clone 1 assessed as reduction of cell death treated for 7 days with replenishment of medium for every 48 hrs by MTT assay (Rvb = 4.4 uM)
    		[PMID: 33691794]
    HCC4006 IC50
    0.47 μM
    Compound: Chemical probe: MS023
    Antiproliferative against human HCC4006 cells expressing MTAP clone 1 assessed as reduction of cell death treated for 7 days with replenishment of medium for every 48 hrs by MTT assay (Rvb = 0.24 uM)
    Antiproliferative against human HCC4006 cells expressing MTAP clone 1 assessed as reduction of cell death treated for 7 days with replenishment of medium for every 48 hrs by MTT assay (Rvb = 0.24 uM)
    		[PMID: 33691794]
    HCC4006 IC50
    0.56 μM
    Compound: Chemical probe: MS023
    Antiproliferative against human HCC4006 cells expressing MTAP clone 2 assessed as reduction of cell death treated for 7 days with replenishment of medium for every 48 hrs by MTT assay (Rvb = 0.24 uM)
    Antiproliferative against human HCC4006 cells expressing MTAP clone 2 assessed as reduction of cell death treated for 7 days with replenishment of medium for every 48 hrs by MTT assay (Rvb = 0.24 uM)
    		[PMID: 33691794]
    SK-LU-1 IC50
    36.7 μM
    Compound: Chemical probe: MS023
    Antiproliferative against human SK-LU-1 cells expressing MTAP clone 1 assessed as reduction of cell death treated for 7 days with replenishment of medium for every 48 hrs by MTT assay (Rvb = 16.3 uM)
    Antiproliferative against human SK-LU-1 cells expressing MTAP clone 1 assessed as reduction of cell death treated for 7 days with replenishment of medium for every 48 hrs by MTT assay (Rvb = 16.3 uM)
    		[PMID: 33691794]
    SK-LU-1 IC50
    41 μM
    Compound: Chemical probe: MS023
    Antiproliferative against human SK-LU-1 cells expressing MTAP clone 2 assessed as reduction of cell death treated for 7 days with replenishment of medium for every 48 hrs by MTT assay (Rvb = 16.3 uM)
    Antiproliferative against human SK-LU-1 cells expressing MTAP clone 2 assessed as reduction of cell death treated for 7 days with replenishment of medium for every 48 hrs by MTT assay (Rvb = 16.3 uM)
    		[PMID: 33691794]
    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.

    MS023 関連抗体

    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).
    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

    287.40

    分子式

    C17H25N3O
    CAS 番号
    Appearance

    Solid

    Color

    White to light yellow

    SMILES

    CN(CCN)CC1=CNC=C1C2=CC=C(OC(C)C)C=C2
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : 100 mg/mL (347.95 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.4795 mL 17.3974 mL 34.7947 mL
    5 mM 0.6959 mL 3.4795 mL 6.9589 mL
    10 mM 0.3479 mL 1.7397 mL 3.4795 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

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

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始）

    C1

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    体積 （開始）

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    体内:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    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:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (8.70 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (8.70 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    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:  Saline

      Solubility: 53.33 mg/mL (185.56 mM); Clear solution; Need ultrasonic and adjust pH to 8 with 1M HCl

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

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    mg/kg

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    (per animal)

    g

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    (per animal)

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
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    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    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).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    純度とドキュメンテーション

    純度: 99.93%

    COA (248 KB) HNMR (241 KB) RP-HPLC (244 KB) MS (205 KB)

    取扱説明書 (2659 KB)
    参考文献

    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. 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
    DMSO 1 mM 3.4795 mL 17.3974 mL 34.7947 mL 86.9868 mL
    5 mM 0.6959 mL 3.4795 mL 6.9589 mL 17.3974 mL
    10 mM 0.3479 mL 1.7397 mL 3.4795 mL 8.6987 mL
    15 mM 0.2320 mL 1.1598 mL 2.3196 mL 5.7991 mL
    20 mM 0.1740 mL 0.8699 mL 1.7397 mL 4.3493 mL
    25 mM 0.1392 mL 0.6959 mL 1.3918 mL 3.4795 mL
    30 mM 0.1160 mL 0.5799 mL 1.1598 mL 2.8996 mL
    40 mM 0.0870 mL 0.4349 mL 0.8699 mL 2.1747 mL
    50 mM 0.0696 mL 0.3479 mL 0.6959 mL 1.7397 mL
    60 mM 0.0580 mL 0.2900 mL 0.5799 mL 1.4498 mL
    80 mM 0.0435 mL 0.2175 mL 0.4349 mL 1.0873 mL
    100 mM 0.0348 mL 0.1740 mL 0.3479 mL 0.8699 mL
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    MS023 Related Classifications

    • Molarity Calculator

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

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
    × = ×
    C1   V1   C2   V2
    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:

    MS0231831110-54-3MS 023MS-023Histone MethyltransferaseInhibitorinhibitorinhibit

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    製品名:
    MS023
    製品番号:
    HY-19615
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