RG108

RG108 is a non-nucleoside DNA methyltransferase (DMNT) inhibitor. RG108 effectively blocked DNA methyltransferases in-vitro and does not cause covalent enzyme trapping in human cell lines. 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.