Bioactivity | 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]. |
Invitro | GSK3735967 (0.1-10000 nM) 以剂量依赖性方式抑制 DNMT1 的活性[1]。 |
Name | GSK3735967 |
CAS | 2170136-86-2 |
Formula | C25H31N7OS |
Molar Mass | 477.62 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [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 Crystallography, 2022, 78: a246. |