GSK3484862 (GSK-3484862) is a selective, non-covalent inhibitor of DNMT1, potently inhibits DNMT1 enzymatic activity with IC50 of 0.23 uM.
GSK3484862 showed no inhibition of the family members DNMT3A/3L and DNMT3B/3L, or the assay coupling enzyme Gla1 at 50 uM.
GSK3484862 is chemically stable, did not bind DNA nonspecifically, and resulted in rapidly reversible inhibition of DNMT1.
GSK-3484862 mediates striking demethylation in murine embryonic stem cells (mESCs) with minimal non-specific toxicity.
Cellular engagement of DNMT1 by GSK3484862 resulted in a dose-dependent loss of promoter DNA methylation and marked transcriptional up-regulation of vimentin in HCT-116 cells.
GSK3484862 reprogrammed mouse embryonic fibroblast C3H/10T1/2 cells into functional muscle or fat cells by expression of the Myod1 or Adipoq differentiation marker genes.
