UNC0638

UNC0638 is an inhibitor of G9a and GLP with excellent potency and selectivity over a wide range of epigenetic and non-epigenetic targets. UNC0638 treatment of a variety of cell lines resulted in lower global H3K9me2 levels, equivalent to levels observed for small hairpin RNA knockdown of G9a and GLP with the functional potency of UNC0638 being well separated from its toxicity. UNC0638 markedly reduced the clonogenicity of MCF7 cells, reduced the abundance of H3K9me2 marks at promoters of known G9a-regulated endogenous genes and disproportionately affected several genomic loci encoding microRNAs.

Histone Methyltransferase Inhibitors Related Products:

EPZ005687; GSK343; Tazemetostat; UNC1999; MM-102; SGC0946; SGC2085; OICR-9429; HLCL-61 HCL; GSK591; SGC707; GSK503; EPZ015666; PFI-2 HCl; UNC0642; GSK-126; EPZ004777; GSK3326595; LLY-507; BRD4770; Pinometostat

[1]. Vedadi M, et al. A chemical probe selectively inhibits G9a and GLP methyltransferase activity in cells. Nat Chem Biol. 2011 Jul 10;7(8):566-74.

[2]. Fu L, et al. Effects of the Histone Methyltransferase Inhibitor UNC0638 on Histone H3K9 Dimethylation of Cultured Ovine Somatic Cells and Development of Resulting Early Cloned Embryos. Reprod Domest Anim. 2014 Apr;49(2):e21-5.