GSK3685032

Catalog No.E1046 Batch:E104603

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Technical Data

Formula

C22H24N6OS
Molecular Weight 420.53 CAS No. 2170137-61-6
Solubility (25°C)* In vitro DMSO 42 mg/mL (99.87 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
0.7mg/ml Taking the 1 mL working solution as an example, add 50 μL of 14 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description GSK3685032 is a non-time-dependent, highly selective enzymatic inhibitor of DNA methyltransferase (DNMT1) with IC50 of 0.036 μM, and over 2500-fold more selective than DNMT3A/3L and DNMT3B/3L.
Targets
DNMT1 [1]
(Cell-free assay)
0.036 μM(ic50)
In vitro

GSK3685032 engages DNMT1 specifically in both biochemical and cellular contexts, and its selective inhibition of DNMT1 slows cancer cell growth. GSK3685032 also induces DNA hypomethylation and gene activation.[1]
In vivo

In mice, GSK3685032 exhibits low clearance, a moderate volume of distribution, and a blood half-life >1.8 h with dose-proportional exposure from 1 to 45 mg/kg, higher doses of GSK3685032 show reductions in neutrophils and red blood cells, these doses showing markedly greater DNA hypomethylation and tumor growth inhibition/regression.[1]

Protocol (from reference)

Animal Study:

[2]
  • Animal Models

    Male C57/BL6 mice

  • Dosages

    2 mg/kg

  • Administration

    s.c.

Selleck's GSK3685032 has been cited by 2 publications

TOPORS E3 ligase mediates resistance to hypomethylating agent cytotoxicity in acute myeloid leukemia cells [ Nat Commun, 2024, 15(1):7360] PubMed: 39198401
UHRF1 is a mediator of KRAS driven oncogenesis in lung adenocarcinoma [ Nat Commun, 2023, 14(1):3966] PubMed: 37407562

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.