"目錄號: HY-13642
RG108 是一種非核苷的 DNA 甲基轉(zhuǎn)移酶 (DNA methyltransferase) 抑制劑，IC50值為 115 nM清酥。
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生物活性
Description
RG108 is a non-nucleoside inhibitor ofDNA methyltransferasewithIC50of 115 nM.
IC50& Target
IC50: 115 nM (DNA methyltransferase)
In Vitro
RG108 effectively blocks DNA methyltransferases in vitro and does not cause covalent enzyme trapping in human cell lines. Incubation of cells with low micromolar concentrations of RG108 results in significant demethylation of genomic DNA without any detectable toxicity. Intriguingly, RG108 causes demethylation and reactivation of tumor suppressor genes, but it does not affect the methylation of centromeric satellite sequences[1]. In another study, the synthesis and in vitro analysis of a biotinylated RG108 conjugate is investigated to evaluate the interactions with DNA methyltransferase enzymes[2]. In a recent study, it is shown RG108 can significantly reduce the DNA methyltransferases activity in SM derived iPS cells as compared to the native SMs[3].
References
