GSK-3484862 is a non-covalent inhibitor for DNA methyltransferase (Dnmt1) . GSK-3484862 induces DNA hypomethylation to against cancer . GSK-3484862 mediates dramatic demethylation in murine embryonic stem cells with minimal non-specific toxicity
In Vitro
GSK-3484862 (0-10 µM, 6 or 14 days) induces dramatic DNA methylation loss. GSK-3484862 (0-10 µM, 4 days) results in a modest reduction in DNMT1 protein level. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: Murine embryonic stem cells (mESC, wild-type (WT) or Dnmt1/3a/3b triple knockout (TKO)) Concentration: 2 µM and 10 µM Incubation Time: 6 or 14 days Result: Induced dramatic DNA methylation loss, with global CpG methylation levels falling from near 70% in WT mESC to less than 18% after 6 days. Western Blot AnalysisCell Line: Murine embryonic stem cells (mESC, wild-type (WT) or Dnmt1/3a/3b triple knockout (TKO)) Concentration: 2 µM and 10 µM Incubation Time: 4 days Result: Resulted in a modest reduction in DNMT1 protein level.
