Home Epigenetics DNA Methyltransferase inhibitor GSK3685032 For research use only.

GSK3685032

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.

GSK3685032 Chemical Structure

GSK3685032 Chemical Structure

CAS No. 2170137-61-6

Purity & Quality Control

Products often used together with GSK3685032

SGI-1027

SGI-1027 is enzymatically less potent and shows decrease in cell-growth inhibition compared to GSK3685032 in MV4-11 cells.

Pappalardi MB, et al. Nat Cancer. 2021 Oct;2(10):1002-1017. Epub 2021 Sep 27.

RG108

GSK3685032 and RG108 non-covalently bind to DNA methyltransferases (DNMTs) active sites, inducing demethylation, transcriptional activation, and cancer cell growth inhibition.

Zheng Q, et al. Int J Mol Sci. 2023 Jun 14;24(12):10130.

CM272

GSK3685032 and CM272 both strongly inhibits DNMT1 with nanomolar activities, but GSK3685032 is stonger than CM272.

JL Medina-Franco, et al. Molecules, 2022, 27(9): 2892.

2'-Deoxy-5-Fluorocytidine

GSK3685032 and 2'-Deoxy-5-Fluorocytidine both inhibit DNMT and induce DNA damage.

GSK3685032 Related Products

Signaling Pathway

DNA Methyltransferase Signaling Pathways

DNA Methyltransferase Signaling Pathway

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
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 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]
Animal Research Animal Models Male C57/BL6 mice
Dosages 2 mg/kg
Administration s.c.

Chemical Information & Solubility

Molecular Weight 420.53 Formula

C22H24N6OS
CAS No. 2170137-61-6 SDF --
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 1 mg/mL ( (2.37 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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