GSK3735967 is a selective, reversible inhibitor of DNA methyltransferase 1 (DNMT1), demonstrating an IC50 value of 40 nM. Featuring a planar dicyanopyridine core, GSK3735967 specifically targets DNMT1 when bound to hemimethylated CpG dinucleotides. Its unique three-binding site configuration allows for interaction with histone H4K20me3, facilitating research into epigenetic regulation and potential therapeutic applications in cancer and other diseases associated with aberrant DNA methylation.
GSK3735967 is a selective, reversible inhibitor of DNA methyltransferase 1 (DNMT1), demonstrating an IC50 value of 40 nM. Featuring a planar dicyanopyridine core, GSK3735967 specifically targets DNMT1 when bound to hemimethylated CpG dinucleotides. Its unique three-binding site configuration allows for interaction with histone H4K20me3, facilitating research into epigenetic regulation and potential therapeutic applications in cancer and other diseases associated with aberrant DNA methylation.
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