RG108

RG108 (N-Phthalyl-L-tryptophan) is a small molecule, non-nucleoside DNA methyltransferase (DNMT) inhibitor. Discovered through structure-based virtual screening, it is designed to block the active site of DNMT enzymes, including DNMT1, DNMT3A, and DNMT3B. Unlike nucleoside analogs such as 5-azacytidine (azacitidine) and decitabine, RG108 does not incorporate into genomic DNA and does not cause DNA damage or covalent enzyme trapping. This profile allows for the induction of global DNA hypomethylation and the reactivation of silenced tumor suppressor genes without the significant cytotoxicity associated with DNA-damaging agents. RG108 is primarily utilized as a high-affinity research tool in epigenetic studies and preclinical oncology research to investigate the mechanisms of gene silencing and cellular differentiation.

Other names

N-Phthalyl-L-tryptophan