GSK-3484862
Based on 26 publication(s) in Google Scholar
GSK-3484862 is a highly potent non-covalent inhibitor and demethylating agent of DNMT1. GSK-3484862 induces genome-wide DNA demethylation, including the regulatory elements of DNMT3B and the promoter region of TERT, and significantly inhibits cell viability, growth, proliferation and self-renewal. GSK-3484862 blocks the transformation of young AT2 cells, induces apoptosis, and generates transcriptomic features similar to those of senescent cells. GSK-3484862 is widely used in studies related to lung cancer, oral squamous cell carcinoma and lung adenocarcinoma.
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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: 99.95%
- CAS 番号: 2170136-65-7
- 分子式: C19H19N5OS
- 分子量:365.45
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
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
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Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 GSK-3484862
More- Nat Genet. 2022 Nov;54(11):1702-1710. [Abstract]
- Nat Commun. 2025 Feb 5;16(1):1377. [Abstract]
- Nat Commun. 2025 Jan 22;16(1):929. [Abstract]
- Nat Commun. 2023 Apr 14;14(1):2122. [Abstract]
- Nat Ecol Evol. 2026 Jun 2. [Abstract]
- Nucleic Acids Res. 2026 Feb 5;54(4):gkag089. [Abstract]
- Nucleic Acids Res. 2024 Sep 23;52(17):10194-10219. [Abstract]
- Nucleic Acids Res. 2024 Mar 21;52(5):e24. [Abstract]
- J Clin Invest. 2023 Apr 17;133(8):e167953. [Abstract]
- Adv Sci (Weinh). 2025 Jan;12(4):e2410360. [Abstract]
- Cell Death Dis. 2025 Apr 4;16(1):251. [Abstract]
- Environ Sci Technol. 2024 Aug 20;58(33):14629-14640. [Abstract]
- Arch Toxicol. 2025 May;99(5):2179-2196. [Abstract]
- Mol Cancer Res. 2022 Nov 3;20(11):1598-1610. [Abstract]
- Drug Dev Res. 2026 May;87(3):e70299. [Abstract]
- J Biochem. 2026 Feb 13:mvag011. [Abstract]
- J Oral Biosci. 2024 Sep;66(3):530-538. [Abstract]
- bioRxiv. 2026 Jun 15.
- bioRxiv. 2026 Feb 8:2026.02.06.704516. [Abstract]
- bioRxiv. 2025 Nov 14.
- bioRxiv. 2025 Oct 20:2025.10.19.683051. [Abstract]
- bioRxiv. 2025 April 08.
- Patent. US20240252638A1.
- biorxiv. 2024 Jun 07.
- bioRxiv. 2024 Apr 3:2024.04.03.587980. [Abstract]
- bioRxiv. September 13, 2021.
Customer Validation & Images
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Bio/Physico-chemical Assay
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IF
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Bio/Physico-chemical Assay
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RT-PCR
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Flow Cytometry
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
製品説明
IC50 & Target
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DNMT1 |
体外実験
GSK-3484862 (2 μM, 10 μM; 6 days) induces global DNA demethylation in mouse embryonic stem cells, reducing the global CpG methylation level of the cells from nearly 70% to less than 18%, and the methylation pattern after induction is similar to that of Dnmt1-/- deficient mouse embryonic stem cells[1].
GSK-3484862 (1-10 μM; 1 week) inhibits proliferation, promotes apoptosis, and reduces the self-renewal capacity of Cal27 and FaDu oral squamous cell carcinoma (OSCC) cells by downregulating the expression of DNMT1[2].
GSK-3484862 inhibits the in vitro transformation of primary alveolar type 2 cells isolated from young KP-Cas9 mice, but has no effect on alveolar type 2 cells from aged KP-Cas9 mice, and induces the expression of Nupr1 and Lcn2 in this system[3].
GSK-3484862 induces hypomethylation at specific CpG sites in Nupr1 enhancers (E1, E7, E8), which correlates with upregulated Nupr1 gene expression[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Murine embryonic stem cells (mESC, wild-type (WT) or Dnmt1/3a/3b triple knockout (TKO))
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Concentration:2 µM and 10 µM
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Incubation Time:6 or 14 days
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Result:Induced dramatic DNA methylation loss, with global CpG methylation levels falling from near 70% in WT mESC to less than 18% after 6 days.
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Cell Line:Murine embryonic stem cells (mESC, wild-type (WT) or Dnmt1/3a/3b triple knockout (TKO))
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Concentration:2 µM and 10 µM
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Incubation Time:4 days
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Result:Resulted in a modest reduction in DNMT1 protein level.
体内実験
Systemic administration of GSK-3484862 inhibits the transformation of AT2 cells in young mice, but has no such effect on AT2 cells in aged mice, while it induces the expression of Nupr1 and Lcn2 in cells from both age groups[3].
GSK-3484862 induces pyroptosis of tumor cells in the mouse 4T1 breast cancer model[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 2170136-65-7
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性状 Solid
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分子量 365.45
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分子式 C19H19N5OS
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Color White to light yellow
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SMILES
O=C(N)[C@H](SC1=NC(N(C)C)=C(C#N)C(CC)=C1C#N)C2=CC=CC=C2
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別名
(R)-GSK3482364
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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 1 year -20°C 6 months
Publications (26)
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Journal Impact Factor
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Most Recent
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Nat Genet
DNA sequence and chromatin modifiers cooperate to confer epigenetic bistability at imprinting control regions. [Abstract]2022 Nov;54(11):1702-1710. PMID: 36333500
GSK-3484862 purchased from MedChemExpress. Usage Cited in: Nat Genet. 2022 Nov;54(11):1702-1710. [Abstract]
Flow cytometric analysis of three independent clones with the methylated Airn-CAG reporter after 2 days treatment with the DNA methylation inhibitor GSK-3484862 (10 µM) and untreated and DMSO controls. Measurements were repeated 7 days after washout of the drug to test for reversion of the reporter silencing.
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Nat Commun
A biallelically active embryonic enhancer dictates GNAS imprinting through allele-specific conformations. [Abstract]2025 Feb 5;16(1):1377. PMID: 39910084
GSK-3484862 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 5;16(1):1377. [Abstract]
WT hESCs were treated with a DNTM1 inhibitor (DNMT1i), GSK-3484862, 10 µM for 17 days.
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Nat Commun
Motif distribution and DNA methylation underlie distinct Cdx2 binding during development and homeostasis. [Abstract]2025 Jan 22;16(1):929. PMID: 39843425
GSK-3484862 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Jan 22;16(1):929. [Abstract]
Fluorescence micrographs showing loss of DNA methylation in cells upon treatment with inhibitor GSK-3484862 (10 μM) for 6 days, (4 independent experiments).
GSK-3484862 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Jan 22;16(1):929. [Abstract]
Representative genomic track showing fractional methylation of CpGs within ACTA1 gene body in HCT116 cells. Lollipop plots show 14 consecutive CpGs within 10 random representative amplicon sequences (from > 100× coverage on nanopore amplicon bisulfite sequencing) and their methylation status upon DMSO or GSK-3484862 (10 µM) treatment and 3 days of recovery; average methylation of all sequenced amplicons (>100× coverage) is represented for all treatment conditions in the right panel.
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Nat Commun
2023 Apr 14;14(1):2122. PMID: 37055433 -
Nat Ecol Evol
Gene body methylation suppresses intragenic transcription and permits epigenetic inheritance in a cnidarian. [Abstract]2026 Jun 2. PMID: 42231006 -
Nucleic Acids Res
Single-molecule tracking of DNMT1 in living cells reveals its cell cycle dynamics and its redistribution upon drug treatment. [Abstract]2026 Feb 5;54(4):gkag089. PMID: 41641704 -
Nucleic Acids Res
The C-terminal 4CXXC-type zinc finger domain of CDCA7 recognizes hemimethylated DNA and modulates activities of chromatin remodeling enzyme HELLS. [Abstract]2024 Sep 23;52(17):10194-10219. PMID: 39142653 -
Nucleic Acids Res
Uncovering the roles of DNA hemi-methylation in transcriptional regulation using MspJI-assisted hemi-methylation sequencing. [Abstract]2024 Mar 21;52(5):e24. PMID: 38261991 -
J Clin Invest
The long-range interaction between two GNAS imprinting control regions delineates pseudohypoparathyroidism type 1B pathogenesis. [Abstract]2023 Apr 17;133(8):e167953. PMID: 36853809
GSK-3484862 purchased from MedChemExpress. Usage Cited in: J Clin Invest. 2023 Apr 17;133(8):e167953. [Abstract]
WT hESCs were treated with 2 μM GSK-3484862 for 2 days. Following the removal of GSK3484862, genomic DNA was purified at the indicated time points, and methylation levels at upstream (UP) and downstream (DOWN) of A/B DMR, MCTS2, PEG10, and KCNQ1OT1 were calculated by MSRE-qPCR. The results showed that in the hESCs, methylation levels at the A/B DMR decreased substantially by day 4 following a 2-day treatment with GSK-3484862 (14.1% and 9.2% methylation for the UP and DOWN regions, respectively).
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Adv Sci (Weinh)
Targeted SPP1 Inhibition of Tumor-Associated Myeloid Cells Effectively Decreases Tumor Sizes. [Abstract]2025 Jan;12(4):e2410360. PMID: 39639496 -
Cell Death Dis
Growth factor receptor plasticity drives therapeutic persistence of metastatic breast cancer. [Abstract]2025 Apr 4;16(1):251. PMID: 40185706 -
Environ Sci Technol
Retinal Degeneration Response to Graphene Quantum Dots: Disruption of the Blood-Retina Barrier Modulated by Surface Modification-Dependent DNA Methylation. [Abstract]2024 Aug 20;58(33):14629-14640. PMID: 39102579 -
Arch Toxicol
Integrative genome-wide aberrant DNA methylation and transcriptome analysis identifies diagnostic markers for colorectal cancer. [Abstract]2025 May;99(5):2179-2196. PMID: 40059124 -
Mol Cancer Res
2022 Nov 3;20(11):1598-1610. PMID: 35925047 -
Drug Dev Res
Sustained DNA Hypomethylation Induced by a DNA Methyltransferase 1 Inhibitor Triggers Apoptosis in Thyroid Cancer Cells. [Abstract]2026 May;87(3):e70299. PMID: 42048599 -
J Biochem
2026 Feb 13:mvag011. PMID: 41679964 -
J Oral Biosci
Exploring the Role of DNMT1 in Dental Papilla Cell Fate Specification during Mouse Tooth Germ Development through Integrated Single-Cell Transcriptomics and Bulk RNA Sequencing. [Abstract]2024 Sep;66(3):530-538. PMID: 38942194 -
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bioRxiv
Regulation of BCL11A DNA binding and expression in human erythrocyte precursor HUDEP-2 cells. [Abstract]2026 Feb 8:2026.02.06.704516. PMID: 41822826 -
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bioRxiv
Divergent roles of DNA methylation, TRIM28, and p53 surveillance in human embryonic and trophoblast stem cells. [Abstract]2025 Oct 20:2025.10.19.683051. PMID: 41279747 -
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bioRxiv
2024 Apr 3:2024.04.03.587980. PMID: 38617249 -
溶剤 & 溶解度
体外:
DMSO : 20 mg/mL (54.73 mM; ultrasonic and warming and heat to 60°C; 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.08 mg/mL (5.69 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.08 mg/mL (5.69 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
In Vivo Dissolution Calculator
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.
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参考文献
[1]. Azevedo Portilho N, et al. The DNMT1 inhibitor GSK-3484862 mediates global demethylation in murine embryonic stem cells. Epigenetics Chromatin. 2021;14(1):56. Published 2021 Dec 15. [Content Brief]
[2]. Liu Y, et al. DNMT1-targeting remodeling global DNA hypomethylation for enhanced tumor suppression and circumvented toxicity in oral squamous cell carcinoma. Mol Cancer. 2024;23(1):104. Published 2024 May 16. [Content Brief]
[4]. Chen Q, et al. GSK-3484862, a DNMT1 degrader, promotes DNMT3B expression in lung cancer cells. NAR Cancer. 2025;7(2):zcaf018. Published 2025 May 27. [Content Brief]
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.7364 mL | 13.6818 mL | 27.3635 mL | 68.4088 mL |
| 5 mM | 0.5473 mL | 2.7364 mL | 5.4727 mL | 13.6818 mL | |
| 10 mM | 0.2736 mL | 1.3682 mL | 2.7364 mL | 6.8409 mL | |
| 15 mM | 0.1824 mL | 0.9121 mL | 1.8242 mL | 4.5606 mL | |
| 20 mM | 0.1368 mL | 0.6841 mL | 1.3682 mL | 3.4204 mL | |
| 25 mM | 0.1095 mL | 0.5473 mL | 1.0945 mL | 2.7364 mL | |
| 30 mM | 0.0912 mL | 0.4561 mL | 0.9121 mL | 2.2803 mL | |
| 40 mM | 0.0684 mL | 0.3420 mL | 0.6841 mL | 1.7102 mL | |
| 50 mM | 0.0547 mL | 0.2736 mL | 0.5473 mL | 1.3682 mL |
GSK-3484862 関連分類
HY-135146 関連分類
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