GSK-3484862

GSK-3484862 is a small molecule, selective DNA methyltransferase 1 (DNMT1) inhibitor developed by GSK. Functioning as a hypomethylating agent (HMA), it reduces DNA methylation levels to promote the re-expression of silenced genes, particularly immunogenic cancer-testis antigens (CTAs) such as NY-ESO-1. Preclinical research, notably in glioblastoma (GBM), has demonstrated that GSK-3484862 can sensitize tumor cells to antigen-specific T-cell mediated immunotherapy. Unlike traditional nucleoside analogs like decitabine, GSK-3484862 is designed to achieve effective immunosensitization with limited cytotoxic effects on surrounding immune cells, providing a potential therapeutic advantage in combining epigenetic modulation with immunotherapy.