2170136-86-2

GSK3735967 is an selective, reversible, non-nucleoside inhibitor of DNMT1 with an IC50 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[1][2].

[1] Horton JR, et al. Structural characterization of dicyanopyridine containing DNMT1-selective, non-nucleoside inhibitors. Structure. 2022 Jun 2;30(6):793-802.e5. DOI:10.1016/j.str.2022.03.009
[2] Horton J, et al. Structural Studies of DNMT1-DNA Complexes with a Reversible Series of Dicyanopyridine Containing Selective, Non-Nucleoside Inhibitors[J]. Foundations of Crystallography, 2022, 78: a246.