1. Epigenetics
  2. DNA Methyltransferase
  3. GSK-3685032

GSK-3685032 

Cat. No.: HY-139664
Handling Instructions

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.

GSK-3685032 Chemical Structure

GSK-3685032 Chemical Structure

CAS No. : 2170137-61-6

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5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 580 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1100 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1700 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2500 In-stock
Estimated Time of Arrival: December 31
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Description

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[1].

IC50 & Target

DNMT1[1]

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].

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 Cmax
(ng/mL)
AUC0-8hr
(h*ng/mL)
DNAUC
(h*kg*ng/mL/mg)
Clearance
(mL/min/kg)
Volumedss
(L/kg)
T1/2
(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

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.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
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GSK-3685032
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HY-139664
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