GSK3735967 is an selective, reversible, non-nucleoside inhibitor of DNMT1 bound hemimetlated CpG dinucleotides. GSK3735967 has three binding sites, one of which can bind to histone H4K20me3[1][2].
GSK3735967 (0.1-10000 nM) 以剂量依赖性方式抑制 DNMT1 的活性[1]。
[1]. Horton JR, et al. Structural characterization of dicyanopyridine containing DNMT1-selective, non-nucleoside inhibitors. Structure. 2022 Jun 2;30(6):793-802.e5.
[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 Crystallograp, 2022, 78: a246.