RG108

DNA methylation regulates gene expression in normal and malignant cells. RG108 is a non-nucleoside DNA methyltransferase inhibitor (IC50 = 115 nM in vitro).{17258} It significantly reduces the methylation of genomic DNA in cells at 10 ?M without detectable toxicity, distinguishing it from nucleoside-based inhibitors like 5-azacytidine.{17257,17258} Further, RG108 inhibits DNA methyltransferase activity by blocking the enzyme active site.{17257} Through these actions, RG108 demethylates and reactivates epigenetically silenced tumor suppressor genes.{17258}