"目录号: HY-13642
Epigenetics-
RG108 是一种非核苷的 DNA 甲基转移酶 (DNA methyltransferase) 抑制剂，IC50值为 115 nM。
DNA Methyltransferase
相关产品
Decitabine-(-)-Epigallocatechin Gallate-SGI-1027-Zebularine-Parthenolide-6-Thioguanine-Lomeguatrib-DC_517-DC_05-N-Acetylprocainamide-Glucose-conjugated MGMT inhibitor-Hinokitiol-γ-Oryzanol-
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
[1].Brueckner B, et al. Epigenetic reactivation of tumor suppressor genes by a novel small-molecule inhibitor of human DNA methyltransferases. Cancer Res. 2005 Jul 15;65(14):6305-11.
[2].Schirrmacher E, et al. Synthesis and in vitro evaluation of biotinylated RG108: a high affinity compound for studying binding interactions with human DNA methyltransferases. Bioconjug Chem. 2006 Mar-Apr;17(2):261-6.
[3].Pasha Z, et al. Efficient non-viral reprogramming of myoblasts to stemness with a single small molecule to generate cardiac progenitor cells. PLoS One. 2011;6(8):e23667.