MS117 is a First-in-Class and Irreversible PRMT6 Covalent Inhibitor
PRMT6 is a protein arginine methyltransferase responsible for histone H3 arginine 2 (H3R2) methylation. PRMT6 negatively regulates DNA methylation and that PRMT6 upregulation contributes to global DNA hypomethylation in cancer. Mechanistically, PRMT6 overexpression impairs the chromatin association of UHRF1, resulting in passive DNA demethylation. Especially, PRMT6 plays an important...
A-366 is a Potent Histone Methyltransferase G9a Inhibitor
Epigenetic alterations to the genome take place via modifications to the DNA or histones. Meanwhile, those modifications lead to changes in gene expression. Generally, histone lysine methylation is a prominent kind of epigenetic regulation for change of the structure chromatin and gene expression. HMTs have recently generated increasing interest...
OTS186935 is a Protein Methyltransferase SUV39H2 Inhibitor
SUV39H2 (Suppressor of variegation 3-9 homolog 2), also known as KMT1B, is a member of the SUV39 subfamily of lysine methyltransferases (KMTs). SUV39H2 results in heterochromatin formation and transcriptional repression. In addition, it is report that SUV39H2 methylate histone H2AX at lysine 134 and enhance the formation of phosphorylated...