GSK-3685032
Based on 15 publication(s) in Google Scholar
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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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.41%
- CAS 番号: 2170137-61-6
- 分子式: C22H24N6OS
- 分子量:420.53
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 GSK-3685032
More- Cell. 2026 Jun 11;189(12):3541-3552.e18. [Abstract]
- Sci Immunol. 2025 Mar 7;10(105):eado9933. [Abstract]
- J Crohns Colitis. 2026 Feb 5;20(2):jjag003. [Abstract]
- NPJ Breast Cancer. 2023 Aug 11;9(1):66. [Abstract]
- Stem Cell Res Ther. 2025 Jul 18;16(1):389. [Abstract]
- J Med Chem. 2024 Sep 12;67(17):15098-15117. [Abstract]
- J Cell Biol. 2024 Apr 1;223(4):e202307026. [Abstract]
- Clin Epigenetics. 2025 Jul 3;17(1):114. [Abstract]
- Res Sq. 2026 May 4.
- University of Rochester. 2025.
- bioRxiv. 2025 Jul 31:2025.07.28.666975. [Abstract]
- Patent. US20250152731A1.
- bioRxiv. 2024 November 06.
- bioRxiv. 2024 Apr 3:2024.04.03.587980. [Abstract]
- bioRxiv. 2023 May 9.
Customer Validation & Images
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Cell Proliferation/Viability Assay
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IF
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Cell Proliferation/Viability Assay
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Flow Cytometry
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WB
DNA Methyltransferase アイソフォーム固有の製品をすべて表示
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生物活性
DNMT1[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HL-60 | IC50 |
0.32 μM
Compound: GSK3685032 ; GSK5032
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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
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[PMID: 39264152] |
| Kasumi 1 | IC50 |
0.38 μM
Compound: GSK3685032 ; GSK5032
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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
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[PMID: 39264152] |
| MV4-11 | IC50 |
>5 μM
Compound: GSK3685032 ; GSK5032
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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
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[PMID: 39264152] |
| MV4-11 | IC50 |
0.4 μM
Compound: GSK3685032 ; GSK5032
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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
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[PMID: 39264152] |
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.
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Cell Line:15 leukemia, 29 lymphoma and 7 multiple myeloma cell lines, e.g., EOL-1, Ki-JK, MM.IR cells.
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Concentration:0.01-100 μM
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Incubation Time:6 days
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Result:Showed cell growth inhibition of majority cancer cell lines, with a median growth IC50 value of 0.64 μM.
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Cell Line:MV4-11 cells
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Concentration:0.1-1000 nM
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Incubation Time:1-6 days
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Result:Exhibited growth inhibition after 3 days, with decreasing growth IC50 throughout a 6 d time course.
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Cell Line:MV4-11 cells
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Concentration:10-10000 nM
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Incubation Time:4 days
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Result:Dose-dependent increased of CXCL11, IFI27, HLA-DQA1 and MAGEA4 following treatment of MV4-11 cells.
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Cell Line:GDM-1 cells
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Concentration:3.2-10,000 nM
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Incubation Time:2 days
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Result:Inhibited DNMT1 protein expression
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.
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Animal Model:MV4-11 xenograft models (female CD1-Foxn1
mice, 12 weeks of age) or SKM-1 xenograft models (NOD. CB17-Prkdc 1NCrCrl 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)
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Administration:Subcutaneous injection, twice daily for 4 weeks
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Result:Revealed statistically significant dose-dependent tumor growth inhibition with clear regression at ≥30 mg/kg.
化学情報
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CAS 番号 2170137-61-6
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性状 Solid
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分子量 420.53
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分子式 C22H24N6OS
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Color White to off-white
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SMILES
N#CC1=C(SC(C2=CC=CC=C2)C(N)=O)N=C(N3CCC(CC3)N)C(C#N)=C1CC
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (15)
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Journal Impact Factor
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Most Recent
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Cell
2026 Jun 11;189(12):3541-3552.e18. PMID: 41999746 -
Sci Immunol
2025 Mar 7;10(105):eado9933. PMID: 40053603 -
J Crohns Colitis
Intermittent ketogenic diet promotes Treg differentiation and alleviates Crohn's disease via the β-hydroxybutyrate driven AHCY-DNMT1-Foxp3 axis. [Abstract]2026 Feb 5;20(2):jjag003. PMID: 41527294 -
NPJ Breast Cancer
Epigenetically upregulating TROP2 and SLFN11 enhances therapeutic efficacy of TROP2 antibody drug conjugate sacitizumab govitecan. [Abstract]2023 Aug 11;9(1):66. PMID: 37567892
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.
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Stem Cell Res Ther
Highly efficient XIST reactivation in female hPSC by transient dual inhibition of TP53 and DNA methylation during Cas9 mediated genome editing. [Abstract]2025 Jul 18;16(1):389. PMID: 40682144
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.
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J Med Chem
Discovery of a Novel Benzimidazole Derivative Targeting Histone Deacetylase to Induce Ferroptosis and Trigger Immunogenic Cell Death. [Abstract]2024 Sep 12;67(17):15098-15117. PMID: 39145486 -
J Cell Biol
Tunable DNMT1 degradation reveals DNMT1/DNMT3B synergy in DNA methylation and genome organization. [Abstract]2024 Apr 1;223(4):e202307026. PMID: 38376465 -
Clin Epigenetics
Exposing the DNA methylation-responsive compartment of the leukaemic genome in T-ALL cell lines support its potential as a novel therapeutic target in T-ALL. [Abstract]2025 Jul 3;17(1):114. PMID: 40611304
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.
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bioRxiv
2025 Jul 31:2025.07.28.666975. PMID: 40766615 -
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bioRxiv
2024 Apr 3:2024.04.03.587980. PMID: 38617249 -
溶剤 & 溶解度
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)
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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.
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.
Please enter the basic information of animal experiments:
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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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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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データシート (283 KB)
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- Français - FR (251 KB)
- Deutsch - DE (251 KB)
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- Español - ES (251 KB)
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- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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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 |
GSK-3685032 関連分類
HY-139664 関連分類
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