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Chemical Structure| 2170137-61-6 Chemical Structure| 2170137-61-6

Structure of GSK-3685032
CAS No.: 2170137-61-6

Chemical Structure| 2170137-61-6

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GSK-3685032 is a non-time-dependent, non-covalent, reversible selective inhibitor of DNMT1 with an IC50 of 0.036 μM. GSK-3685032 induces DNA demethylation, transcriptional activation, and inhibition of cancer cell growth.

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Product Details of GSK-3685032

CAS No. :2170137-61-6
Formula : C22H24N6OS
M.W : 420.53
SMILES Code : O=C(N)C(SC1=NC(N2CCC(N)CC2)=C(C#N)C(CC)=C1C#N)C3=CC=CC=C3
MDL No. :N/A

Safety of GSK-3685032

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319
Precautionary Statements:P501-P270-P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313-P301+P312+P330

Related Pathways of GSK-3685032

epigenetics

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
ES-2 100 nM, 500 nM, 1 μM, or 5 μM 1, 2, or 4 days To evaluate the effect of GSK-3685032 on ORF1p expression in ES-2 cells, results showed that GSK-3685032 robustly induced ORF1p expression within 4 days without appreciable DNA damage. NPJ Precis Oncol. 2025 Mar 6;9(1):62
12Z 100 nM, 500 nM, 1 μM, or 5 μM 1, 2, or 4 days To evaluate the effect of GSK-3685032 on ORF1p expression in 12Z cells, results showed that GSK-3685032 robustly induced ORF1p expression within 4 days without appreciable DNA damage. NPJ Precis Oncol. 2025 Mar 6;9(1):62
hEM3 100 nM, 500 nM, 1 μM, or 5 μM 1, 2, or 4 days To evaluate the effect of GSK-3685032 on ORF1p expression in hEM3 cells, results showed that GSK-3685032 robustly induced ORF1p expression within 4 days without appreciable DNA damage. NPJ Precis Oncol. 2025 Mar 6;9(1):62
KRAS mutant NSCLC cells 10 nM Evaluate the effect of DNMT1 inhibition on 3D growth, results showed similar to UHRF1 knockout, significantly inhibiting spheroid growth Nat Commun. 2023 Jul 5;14(1):3966
MDS-L cells 1 µM 4 days To assess the sensitivity of MDS-L cells to GSK-3685032, results showed no significant difference in sensitivity between TOPORS-edited and control cells. Nat Commun. 2024 Aug 28;15(1):7360

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice MV4–11 and SKM-1 subcutaneous xenograft models Subcutaneous injection 1 to 45 mg/kg Twice daily for ≥4 weeks To evaluate the in vivo efficacy and tolerability of GSK3685032 in AML models Nat Cancer. 2021 Oct;2(10):1002-1017

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Bio Calculators
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1 mM

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10 mM

2.38mL

0.48mL

0.24mL

11.89mL

2.38mL

1.19mL

23.78mL

4.76mL

2.38mL

 

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