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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GSK-3484862 Chemical Structure

GSK-3484862 Chemical Structure

CAS No. : 2170136-65-7

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 275 In-stock
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10 mM * 1 mL in DMSO USD 275 In-stock
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1 mg USD 55 In-stock
5 mg USD 150 In-stock
10 mg USD 250 In-stock
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Based on 11 publication(s) in Google Scholar

Other Forms of GSK-3484862:

GSK-3484862 Related Antibodies

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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

Light yellow to 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 : 20.83 mg/mL (57.00 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 2.7364 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
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Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
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
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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