2. Epigenetics
  3. DNA Methyltransferase
  4. GSK-3685032

GSK-3685032 is a non-time-dependent, noncovalently, first-in-class reversible DNMT1-selective inhibitor, with an IC50 of 0.036 μM. GSK-3685032 induces robust loss of DNA methylation, transcriptional activation, and cancer cell growth inhibition.

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CAS 番号 : 2170137-61-6

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 242 在庫あり
Solution
10 mM * 1 mL in DMSO USD 242 在庫あり
Solid
1 mg $90 在庫あり
5 mg $220 在庫あり
10 mg $350 在庫あり
25 mg $700 在庫あり
50 mg $1050 在庫あり
100 mg $1570 在庫あり
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カスタマーレビュー

Based on 13 publication(s) in Google Scholar

Other Forms of GSK-3685032:

GSK-3685032 関連抗体

Top Publications Citing Use of Products

    GSK-3685032 purchased from MedChemExpress. Usage Cited in: Stem Cell Res Ther. 2025 Jul 18;16(1):389.  [Abstract]

    GSK3685032 (0.5, 1, 5 μM) treatment resulted in dose-dependent growth inhibition, with most cells dying after two weeks.

    GSK-3685032 purchased from MedChemExpress. Usage Cited in: Stem Cell Res Ther. 2025 Jul 18;16(1):389.  [Abstract]

    DNAme levels were signifcantly reduced upon GSK3685032 (1 μM, 120 h) treatmen by immunofuorescence (IF) analysis.

    GSK-3685032 purchased from MedChemExpress. Usage Cited in: Clin Epigenetics. 2025 Jul 3;17(1):114.  [Abstract]

    Cell viability as percentage of untreated control for eleven T-ALL cells treated with GSK-3685032 (10, 100, 1000, 10000 nM) for 3 and 7 days.

    GSK-3685032 purchased from MedChemExpress. Usage Cited in: Clin Epigenetics. 2025 Jul 3;17(1):114.  [Abstract]

    Percentage of dead cells (apoptotic and necrotic) after treatment of JURKAT and SUP-T1 cells with indicated concentrations of GSK5032 (300 nM) for 3 days based on flow cytometry analysis.

    GSK-3685032 purchased from MedChemExpress. Usage Cited in: NPJ Breast Cancer. 2023 Aug 11;9(1):66.  [Abstract]

    Breast cancer cell lines were treated with GSK-3685032 at 10 μM and decitabine at 1 µM for 3 days. DNMT1 and TROP2 levels were examined by immunoblotting.

    DNA 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
    DNA Methyltransferase DNMT1 DNMT3 MGMT

    • 生物活性

    • 純度とドキュメンテーション

    • 参考文献

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    製品説明

    GSK-3685032 is a non-time-dependent, noncovalently, first-in-class reversible DNMT1-selective inhibitor, with an IC50 of 0.036 μM. GSK-3685032 induces robust loss of DNA methylation, transcriptional activation, and cancer cell growth inhibition[1].

    IC50 & Target

    DNMT1[1]
    Cellular Effect
    Cell Line Type Value Description References
    HL-60 IC50
    0.32 μM
    Compound: GSK3685032 ; GSK5032
    Inhibition of cell viability in human HL-60 cells incubated for 4 days in presence of SAHA by CCK8 assay
    Inhibition of cell viability in human HL-60 cells incubated for 4 days in presence of SAHA by CCK8 assay
    		[PMID: 39264152]
    Kasumi 1 IC50
    0.38 μM
    Compound: GSK3685032 ; GSK5032
    Inhibition of cell viability in human Kasumi 1 cells incubated for 4 days in presence of SAHA by CCK8 assay
    Inhibition of cell viability in human Kasumi 1 cells incubated for 4 days in presence of SAHA by CCK8 assay
    		[PMID: 39264152]
    MV4-11 IC50
    >5 μM
    Compound: GSK3685032 ; GSK5032
    Antiproliferative activity against human MV4-11 cells incubated for 96 hrs by CCK8 assay
    Antiproliferative activity against human MV4-11 cells incubated for 96 hrs by CCK8 assay
    		[PMID: 39264152]
    MV4-11 IC50
    0.4 μM
    Compound: GSK3685032 ; GSK5032
    Inhibition of cell viability in human MV4-11 cells incubated for 4 days in presence of SAHA by CCK8 assay
    Inhibition of cell viability in human MV4-11 cells incubated for 4 days in presence of SAHA by CCK8 assay
    		[PMID: 39264152]
    体外実験

    GSK-3685032 (6 days) has cell growth inhibition of majority cancer cell lines, with a median growth IC50 value of 0.64 μM[1].
    GSK-3685032 (0.1-1000 nM, 1-6 days) exhibits growth inhibition after 3 days, with decreasing growth IC50 throughout a 6 d time course[1].
    GSK3685032 (10-10000 nM, day 4) dose-dependently increases the immune-related gene transcription[1].
    GSK3685032 (3.2-10,000 nM, 2 days) inhibits DNMT1 protein expression[1].
    GSK3685032 induces DNA hypomethylation and gene activation[1].

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

    GSK-3685032 関連抗体

    Cell Proliferation Assay[1]

    Cell Line: 15 leukemia, 29 lymphoma and 7 multiple myeloma cell lines, e.g., EOL-1, Ki-JK, MM.IR cells.
    Concentration: 0.01-100 μM
    Incubation Time: 6 days
    Result: Showed cell growth inhibition of majority cancer cell lines, with a median growth IC50 value of 0.64 μM.

    Cell Proliferation Assay[1]

    Cell Line: MV4-11 cells
    Concentration: 0.1-1000 nM
    Incubation Time: 1-6 days
    Result: Exhibited growth inhibition after 3 days, with decreasing growth IC50 throughout a 6 d time course.

    RT-PCR[1]

    Cell Line: MV4-11 cells
    Concentration: 10-10000 nM
    Incubation Time: 4 days
    Result: Dose-dependent increased of CXCL11, IFI27, HLA-DQA1 and MAGEA4 following treatment of MV4-11 cells.

    Western Blot Analysis[1]

    Cell Line: GDM-1 cells
    Concentration: 3.2-10,000 nM
    Incubation Time: 2 days
    Result: Inhibited DNMT1 protein expression
    体内実験

    GSK-3685032 (1-45 mg/kg; subcutaneous twice daily for 28 days) inhibits tumor growth in the subcutaneous MV4-11 or SKM-1 xenograft models[1].

    Summary of mouse pharmacokinetic parameters for GSK-3685032[1]

    Dose,Route Cmax
    (ng/mL)    		 AUC0-8hr
    (h*ng/mL)    		 DNAUC
    (h*kg*ng/mL/mg)    		 Clearance
    (mL/min/kg)    		 Volumedss
    (L/kg)    		 T1/2
    (h)
    2 mg/kg,IV 5103 2418 1209 13 1.3 1.8
    2 mg/kg,SC 252 921 461 NA NA 2.8
    2 mg/kg,SC 5473 15400 513 NA NA ND

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

    Animal Model: MV4-11 xenograft models (female CD1-Foxn1 mice, 12 weeks of age) or SKM-1 xenograft models (NOD. CB17-Prkdc1NCrCrl mice, 8-11 weeks of age)[1]
    Dosage: 1, 5, 15, 30, 45 mg/kg (10% captisol adjusted to pH 4.5-5 with 1 M acetic acid, stored for up to 1 week at 4 °C)
    Administration: Subcutaneous injection, twice daily for 4 weeks
    Result: Revealed statistically significant dose-dependent tumor growth inhibition with clear regression at ≥30 mg/kg.
    分子量

    420.53

    分子式

    C22H24N6OS
    CAS 番号
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    N#CC1=C(SC(C2=CC=CC=C2)C(N)=O)N=C(N3CCC(CC3)N)C(C#N)=C1CC
    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 : 25 mg/mL (59.45 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 2.3780 mL 11.8898 mL 23.7795 mL
    5 mM 0.4756 mL 2.3780 mL 4.7559 mL
    10 mM 0.2378 mL 1.1890 mL 2.3780 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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    一般には略語で表示されます：C1V1 = C2V2

    濃度 （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    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (5.94 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 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    In Vivo Dissolution Calculator
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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: 99.41%

    COA (253 KB) HNMR (291 KB) LCMS (94 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.3780 mL 11.8898 mL 23.7795 mL 59.4488 mL
    5 mM 0.4756 mL 2.3780 mL 4.7559 mL 11.8898 mL
    10 mM 0.2378 mL 1.1890 mL 2.3780 mL 5.9449 mL
    15 mM 0.1585 mL 0.7927 mL 1.5853 mL 3.9633 mL
    20 mM 0.1189 mL 0.5945 mL 1.1890 mL 2.9724 mL
    25 mM 0.0951 mL 0.4756 mL 0.9512 mL 2.3780 mL
    30 mM 0.0793 mL 0.3963 mL 0.7927 mL 1.9816 mL
    40 mM 0.0594 mL 0.2972 mL 0.5945 mL 1.4862 mL
    50 mM 0.0476 mL 0.2378 mL 0.4756 mL 1.1890 mL
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    GSK-3685032 Related Classifications

    • Molarity Calculator

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    The dilution calculator equation

    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:

    GSK-36850322170137-61-6GSK3685032GSK 3685032DNA MethyltransferaseDNMTsDNA MTasesleukemialymphomamultiple myelomaMV4–11GDM-1cancerInhibitorinhibitorinhibit

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    製品名:
    GSK-3685032
    製品番号:
    HY-139664
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