GSK-3685032

Name: GSK-3685032
Brand: MedChemExpress
SKU: HY-139664
Rating: 5.0 (13 reviews)

Cat. No.: HY-139664 Purity: 99.41%: Data Sheet
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GSK-3685032 is a non-time-dependent, noncovalently, first-in-class reversible DNMT1-selective inhibitor, with an IC₅₀ of 0.036 μM. GSK-3685032 induces robust loss of DNA methylation, transcriptional activation, and cancer cell growth inhibition.

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

CAS No. : 2170137-61-6

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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Customer Review

Based on 13 publication(s) in Google Scholar

Other Forms of GSK-3685032:

(R)-GSK-3685032 In-stock
(S)-GSK-3685032 In-stock

13 Publications Citing Use of MCE GSK-3685032

Cell Proliferation/Viability Assay

Flow Cytometry

: GSK-3685032 purchased from MedChemExpress. Usage Cited in: Stem Cell Res Ther. 2025 Jul 18;16(1):389. [Abstract]; GSK3685032 (0.5, 1, 5 μM) treatment resulted in dose-dependent growth inhibition, with most cells dying after two weeks.

: GSK-3685032 purchased from MedChemExpress. Usage Cited in: Stem Cell Res Ther. 2025 Jul 18;16(1):389. [Abstract]; DNAme levels were signifcantly reduced upon GSK3685032 (1 μM, 120 h) treatmen by immunofuorescence (IF) analysis.

: GSK-3685032 purchased from MedChemExpress. Usage Cited in: Clin Epigenetics. 2025 Jul 3;17(1):114. [Abstract]; Cell viability as percentage of untreated control for eleven T-ALL cells treated with GSK-3685032 (10, 100, 1000, 10000 nM) for 3 and 7 days.

: GSK-3685032 purchased from MedChemExpress. Usage Cited in: Clin Epigenetics. 2025 Jul 3;17(1):114. [Abstract]; Percentage of dead cells (apoptotic and necrotic) after treatment of JURKAT and SUP-T1 cells with indicated concentrations of GSK5032 (300 nM) for 3 days based on flow cytometry analysis.

: GSK-3685032 purchased from MedChemExpress. Usage Cited in: NPJ Breast Cancer. 2023 Aug 11;9(1):66. [Abstract]; Breast cancer cell lines were treated with GSK-3685032 at 10 μM and decitabine at 1 µM for 3 days. DNMT1 and TROP2 levels were examined by immunoblotting.

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DNA Methyltransferase DNMT1 DNMT3 MGMT

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

DNMT1^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
HL-60	IC₅₀	0.32 μM Compound: GSK3685032 ; GSK5032	Inhibition of cell viability in human HL-60 cells incubated for 4 days in presence of SAHA by CCK8 assay Inhibition of cell viability in human HL-60 cells incubated for 4 days in presence of SAHA by CCK8 assay	[PMID: 39264152]
Kasumi 1	IC₅₀	0.38 μM Compound: GSK3685032 ; GSK5032	Inhibition of cell viability in human Kasumi 1 cells incubated for 4 days in presence of SAHA by CCK8 assay Inhibition of cell viability in human Kasumi 1 cells incubated for 4 days in presence of SAHA by CCK8 assay	[PMID: 39264152]
MV4-11	IC₅₀	0.4 μM Compound: GSK3685032 ; GSK5032	Inhibition of cell viability in human MV4-11 cells incubated for 4 days in presence of SAHA by CCK8 assay Inhibition of cell viability in human MV4-11 cells incubated for 4 days in presence of SAHA by CCK8 assay	[PMID: 39264152]
MV4-11	IC₅₀	> 5 μM Compound: GSK3685032 ; GSK5032	Antiproliferative activity against human MV4-11 cells incubated for 96 hrs by CCK8 assay Antiproliferative activity against human MV4-11 cells incubated for 96 hrs by CCK8 assay	[PMID: 39264152]

In Vitro

GSK-3685032 (6 days) has cell growth inhibition of majority cancer cell lines, with a median growth IC₅₀ value of 0.64 μM^[1].
GSK-3685032 (0.1-1000 nM, 1-6 days) exhibits growth inhibition after 3 days, with decreasing growth IC₅₀ throughout a 6 d time course^[1].
GSK3685032 (10-10000 nM, day 4) dose-dependently increases the immune-related gene transcription^[1].
GSK3685032 (3.2-10,000 nM, 2 days) inhibits DNMT1 protein expression^[1].
GSK3685032 induces DNA hypomethylation and gene activation^[1].

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

Cell Proliferation Assay^[1]

Cell Line:	15 leukemia, 29 lymphoma and 7 multiple myeloma cell lines, e.g., EOL-1, Ki-JK, MM.IR cells.
Concentration:	0.01-100 μM
Incubation Time:	6 days
Result:	Showed cell growth inhibition of majority cancer cell lines, with a median growth IC₅₀ value of 0.64 μM.

Cell Proliferation Assay^[1]

Cell Line:	MV4-11 cells
Concentration:	0.1-1000 nM
Incubation Time:	1-6 days
Result:	Exhibited growth inhibition after 3 days, with decreasing growth IC₅₀ throughout a 6 d time course.

RT-PCR^[1]

Cell Line:	MV4-11 cells
Concentration:	10-10000 nM
Incubation Time:	4 days
Result:	Dose-dependent increased of CXCL11, IFI27, HLA-DQA1 and MAGEA4 following treatment of MV4-11 cells.

Western Blot Analysis^[1]

Cell Line:	GDM-1 cells
Concentration:	3.2-10,000 nM
Incubation Time:	2 days
Result:	Inhibited DNMT1 protein expression

In Vivo

GSK-3685032 (1-45 mg/kg; subcutaneous twice daily for 28 days) inhibits tumor growth in the subcutaneous MV4-11 or SKM-1 xenograft models^[1].

Summary of mouse pharmacokinetic parameters for GSK-3685032^[1]

Dose,Route	C_max (ng/mL)	AUC_0-8hr (h*ng/mL)	DNAUC (hkgng/mL/mg)	Clearance (mL/min/kg)	Volume_dss (L/kg)	T_1/2 (h)
2 mg/kg,IV	5103	2418	1209	13	1.3	1.8
2 mg/kg,SC	252	921	461	NA	NA	2.8
2 mg/kg,SC	5473	15400	513	NA	NA	ND

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

Animal Model:	MV4-11 xenograft models (female CD1-Foxn1 mice, 12 weeks of age) or SKM-1 xenograft models (NOD. CB17-Prkdc1NCrCrl mice, 8-11 weeks of age)^[1]
Dosage:	1, 5, 15, 30, 45 mg/kg (10% captisol adjusted to pH 4.5-5 with 1 M acetic acid, stored for up to 1 week at 4 °C)
Administration:	Subcutaneous injection, twice daily for 4 weeks
Result:	Revealed statistically significant dose-dependent tumor growth inhibition with clear regression at ≥30 mg/kg.

Molecular Weight

420.53

Formula

C₂₂H₂₄N₆OS

CAS No.

2170137-61-6

Appearance

Solid

Color

White to off-white

SMILES

N#CC1=C(SC(C2=CC=CC=C2)C(N)=O)N=C(N3CCC(CC3)N)C(C#N)=C1CC

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 25 mg/mL (59.45 mM; Need ultrasonic; 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	2.3780 mL	11.8898 mL	23.7795 mL
5 mM	0.4756 mL	2.3780 mL	4.7559 mL
10 mM	0.2378 mL	1.1890 mL	2.3780 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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: ≥ 2.5 mg/mL (5.94 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.41%

Select Batch:

Data Sheet (283 KB) SDS (251 KB)

COA (253 KB) HNMR (291 KB) LCMS (94 KB)

Handling Instructions (2659 KB)

References

[1]. Pappalardi MB, et al. Discovery of a first-in-class reversible DNMT1-selective inhibitor with improved tolerability and efficacy in acute myeloid leukemia. Nat Cancer. 2021;2(10):1002-1017. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.3780 mL	11.8898 mL	23.7795 mL	59.4488 mL
	5 mM	0.4756 mL	2.3780 mL	4.7559 mL	11.8898 mL
	10 mM	0.2378 mL	1.1890 mL	2.3780 mL	5.9449 mL
	15 mM	0.1585 mL	0.7927 mL	1.5853 mL	3.9633 mL
	20 mM	0.1189 mL	0.5945 mL	1.1890 mL	2.9724 mL
	25 mM	0.0951 mL	0.4756 mL	0.9512 mL	2.3780 mL
	30 mM	0.0793 mL	0.3963 mL	0.7927 mL	1.9816 mL
	40 mM	0.0594 mL	0.2972 mL	0.5945 mL	1.4862 mL
	50 mM	0.0476 mL	0.2378 mL	0.4756 mL	1.1890 mL

GSK-3685032 Related Classifications

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.

Keywords:

GSK-36850322170137-61-6GSK3685032GSK 3685032DNA MethyltransferaseDNMTsDNA MTasesleukemialymphomamultiple myelomaMV4–11GDM-1cancerInhibitorinhibitorinhibit

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GSK-3685032

Customer Review

Other Forms of GSK-3685032:

GSK-3685032 Related Antibodies

13 Publications Citing Use of MCE GSK-3685032

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All DNA Methyltransferase Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

GSK-3685032 Related Antibodies

Molarity Calculator

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Complete Stock Solution Preparation Table

GSK-3685032 Related Classifications

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