UNC0631

UNC0631 is a potent and selective small molecule inhibitor of the histone methyltransferases G9a (EHMT2) and G9a-like protein (GLP/EHMT1). Developed at the University of North Carolina at Chapel Hill, it serves as a chemical probe to investigate the epigenetic regulation of gene expression, specifically the dimethylation of histone H3 lysine 9 (H3K9me2). In preclinical research, UNC0631 has shown significant activity in reducing the viability of glioma and glioblastoma cells, including recurrent and treatment-resistant tumor models. Its mechanism involves competitive binding with the substrate, thereby blocking the methyltransferase activity of the G9a/GLP complex, which is often overexpressed in various cancers and associated with gene silencing and tumor progression.