GSK3685032

SKU: orb1298013

Description

GSK3685032 is a potent, selective, and reversible non-covalent inhibitor of DNMT1 (IC50 = 36 nM). It induces DNA demethylation and gene reactivation, demonstrating robust anti-proliferative effects in cancer cell lines and in vivo tumor models, making it a valuable tool for epigenetic and oncology research.

Research Area

Epigenetics & Chromatin

Key Properties

• CAS Number: 2170137-61-6
• MW: 420.53
• Purity: 99.87% (May vary between batches)
• Formula: C₂₂H₂₄N₆OS
• SMILES: CCc1c(C#N)c(SC(C(N)=O)c2ccccc2)nc(N2CCC(N)CC2)c1C#N
• Target: DNA Methyltransferase
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.76 mM);DMSO:26.4 mg/mL (62.78 mM)

Bioactivity

• Target IC50:
  EOL-1 cells:0.64 μM|DNMT1:36 nM|MM.IR cells:0.64 μM|Ki-JK cells:0.64 μM
• In Vivo:
  In MV4-11 xenograft models or SKM-1 xenograft models, GSK-3685032 (1-45 mg/kg; s.c.) inhibited dose-dependent tumor growth with clear regression at ≥30 mg/kg.
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• In Vitro:
  In MV4-11 cells, GSK3685032 (0.1-1000 nM, 1-6 days) exhibited growth inhibition after 3 days, with decreasing growth IC50 throughout a 6 d time course. GSK3685032 (10-10000 nM, day 4) increased the immune-related gene transcription in a dose dependent manner. GSK3685032 (3.2-10,000 nM, 2 days) inhibited DNMT1 protein expression. In 15 leukemia, 29 lymphoma and 7 multiple myeloma cell lines, e.g., EOL-1, Ki-JK, MM.IR cells, GSK3685032 (6 days) showed cell growth inhibition of majority cancer cell lines, with a median growth IC50 value of 0.64 μM. GSK3685032 induced DNA hypomethylation and gene activation.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

cancer, DNA Methyltransferase, DNA MTases, DNAMethyltransferase, DNMT1, DNMTs, GSK3685032, GSK-3685032, GSK 3685032, leukemia, GDM-1, lymphoma, Inhibitor, inhibit, multiple myeloma, MV4–11

Compound Identifiers

PubChem CID

132233067