2. Epigenetics
  3. DNA Methyltransferase
  4. GSK-3484862

GSK-3484862 is a non-covalent inhibitor for DNA methyltransferase (Dnmt1). GSK-3484862 induces DNA hypomethylation to against cancer. GSK-3484862 mediates dramatic demethylation in murine embryonic stem cells with minimal non-specific toxicity.

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CAS No. : 2170136-65-7

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10 mM * 1 mL in DMSO
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Based on 22 publication(s) in Google Scholar

Other Forms of GSK-3484862:

GSK-3484862 Related Antibodies

Top Publications Citing Use of Products

    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.

    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.

    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).

    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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    Description

    GSK-3484862 is a non-covalent inhibitor for DNA methyltransferase (Dnmt1). GSK-3484862 induces DNA hypomethylation to against cancer. GSK-3484862 mediates dramatic demethylation in murine embryonic stem cells with minimal non-specific toxicity[1][2].

    IC50 & Target

    DNMT1

     

    In Vitro

    GSK-3484862 (0-10 μM, 6 or 14 days) induces dramatic DNA methylation loss[2].
    GSK-3484862 (0-10 μM, 4 days) results in a modest reduction in DNMT1 protein level[2].

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

    GSK-3484862 Related Antibodies

    Cell Viability Assay[2]

    Cell Line: Murine embryonic stem cells (mESC, wild-type (WT) or Dnmt1/3a/3b triple knockout (TKO))
    Concentration: 2 µM and 10 µM
    Incubation Time: 6 or 14 days
    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.

    Western Blot Analysis[2]

    Cell Line: Murine embryonic stem cells (mESC, wild-type (WT) or Dnmt1/3a/3b triple knockout (TKO))
    Concentration: 2 µM and 10 µM
    Incubation Time: 4 days
    Result: Resulted in a modest reduction in DNMT1 protein level.
    Molecular Weight

    365.45

    Formula

    C19H19N5OS
    CAS No.
    Appearance

    Solid

    Color

    White to light yellow

    SMILES

    O=C(N)[C@H](SC1=NC(N(C)C)=C(C#N)C(CC)=C1C#N)C2=CC=CC=C2
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

    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)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.7364 mL 13.6818 mL 27.3635 mL
    5 mM 0.5473 mL 2.7364 mL 5.4727 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, 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.

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

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    In Vivo:

    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: 2.08 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.
    • Protocol 2

      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
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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.
    Purity & Documentation

    Purity: 99.95%

    SDS (393 KB)

    COA (252 KB) RP-HPLC (247 KB) LCMS (273 KB)

    Handling Instructions (2659 KB)
    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, 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
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    GSK-3484862 Related Classifications

    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-34848622170136-65-7GSK3484862GSK 3484862DNA MethyltransferaseDNMTsDNA MTasesDNAmethyltransferase1Dnmt1hypomethylationepigenetictherapies5-AzacytidineInhibitorinhibitorinhibit

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