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> GSK-3484862 [2170136-65-7]

GSK-3484862 [2170136-65-7]

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Référence HY-135146-50mg

Conditionnement : 50mg

Marque : MedChemExpress


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.
Masse moléculaire

365.45

Formule

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
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 1 year
-20°C 6 months
Solvant et solubilité
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.

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.
Pureté et documentation
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