REVIEW RG-108 is a non-nucleoside DNA methyltransferase inhibitor (IC50 = 115 nM in vitro). It reduces the methylation of genomic DNA, by blocking the enzyme active site in cells at 10 uM without detectable toxicity, distinguishing it from nucleoside-based inhibitors like 5-azacytidine. RG-108 demethylates and reactivates epigenetically silenced tumor suppressor genes and enhances the efficiency of induced pluripotent stem cell (iPS) generation.
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