RG108

RG108 is a non-nucleoside DNA methyltransferase (DMNT) inhibitor. RG108 effectively blocked DNA methyltransferases in vitro and did not cause covalent enzyme trapping in human cell lines. RG108 also inhibits human tumor cell line (HCT116, NALM-6) proliferation and increased doubling time in culture. RG108 significantly reduces the methylation of genomic DNA in cells at 10 μM without detectable toxicity, distinguishing it from nucleoside-based inhibitors like 5-azacytidine. Through these actions, RG108 demethylates and reactivates epigenetically silenced tumor suppressor genes.