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GSK3685032 DNMT1 Inhibitor

Name: GSK3685032
Brand: Selleck Chemicals
SKU: E1046
Availability: InStock
Rating: 5 (4 reviews)

Cat.No.E1046

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.

Chemical Structure

Molecular Weight: 420.53

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Quality Control

Batch: Purity: 99.99%

99.99

Products Often Used Together with GSK3685032

SGI-1027

In MV4-11 cells, it is enzymatically less potent and shows decreased cell-growth inhibition compared to GSK3685032.

RG108

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

CM272

Both GSK3685032 and CM272 strongly inhibit DNMT1 with nanomolar activities, but it is stronger than CM272.

2'-Deoxy-5-Fluorocytidine

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

Related Targets	HDAC JAK BET Histone Methyltransferase PKC PARP HIF PRMT EZH2 AMPK
Other DNA Methyltransferase Inhibitors	RG108 SGI-1027 Zebularine (NSC 309132) Gamma-Oryzanol CM272 β-thujaplicin GSK-3484862 Bobcat339 DC-05 2'-Deoxy-5-Fluorocytidine

Solubility

In vitro
Batch:

DMSO : 1 mg/mL (2.37 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.700mg/ml (1.66mM)	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.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

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

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	420.53	Formula	C₂₂H₂₄N₆OS	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	2170137-61-6	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent

Mechanism of Action

Targets/IC₅₀/Ki	DNMT1 (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. This compound also induces DNA hypomethylation and gene activation.
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 this compound show reductions in neutrophils and red blood cells, these doses showing markedly greater DNA hypomethylation and tumor growth inhibition/regression.
References	[1] https://pubmed.ncbi.nlm.nih.gov/34790902/ [2] https://pubmed.ncbi.nlm.nih.gov/34790902/

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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