GSK3735967 is an selective, reversible, non-nucleoside inhibitor of DNMT1 with an IC 50 value of 40 nM. GSK3735967 contains a planar dicyanopyridine core that can specifically embed DNMT1 bound hemimethylated CpG dinucleotides. GSK3735967 has three binding sites, one of which can bind to histone H4K20me3.
In Vitro
GSK3735967 (0.1-10000 nM) inhibits the activity of DNMT1 in a dose dependent manner. MCE has not independently confirmed the accuracy of these methods. They are for reference only.