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

GSK-3484862 

Cat. No.: HY-135146 Purity: 99.62%
COA Handling Instructions

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.

For research use only. We do not sell to patients.

GSK-3484862 Chemical Structure

GSK-3484862 Chemical Structure

CAS No. : 2170136-65-7

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 275 In-stock
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 275 In-stock
Solid
1 mg USD 55 In-stock
5 mg USD 150 In-stock
10 mg USD 250 In-stock
50 mg USD 650 In-stock
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Based on 5 publication(s) in Google Scholar

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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].

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

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

Appearance

Solid

Formula

C19H19N5OS
CAS No.
SMILES

O=C(N)[[email protected]](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 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 20.83 mg/mL (57.00 mM; Need ultrasonic)

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
10 mM 0.2736 mL 1.3682 mL 2.7364 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

*All of the co-solvents are available by MCE.
Purity & Documentation
References
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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.

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Keywords:

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

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