GSK3735967

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].

Product Specifications

CAS Number

[2170136-86-2]

UNSPSC

12352005

Target

DNA Methyltransferase

Type

Reference compound

Related Pathways

Epigenetics

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/gsk3735967.html

Concentration

10mM

Purity

99.34

Solubility

DMSO : 31.25 mg/mL (ultrasonic; warming; heat to 70°C)

Smiles

N#CC1=C(SCC2=CC=C(CNC(CN)=O)C=C2)N=C(N3CCN(CCC3)C)C(C#N)=C1CC

Molecular Formula

C25H31N7OS

Molecular Weight

477.62

References & Citations

[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.