中文同义词:
N-酞酰-L-色氨酸;(S)-2-(1,3-二氧代异吲哚啉-2-基)-3-(1H-吲哚-3-基)丙酸;N-邻苯二甲酰基-L-色氨酸;DNA甲基转移酶抑制剂(RG108)
英文同义词:
(S)-2-(1,3-dioxoisoindolin-2-yl)-3-(1H-indol-3-yl)propanoic acid;RG108/RG-108;(S)-3-(Indol-3-yl)-2-(1,3-dihydro-1,3-dioxo-2H-isoindol-2-yl)propanoic acid;N-Phthaloyl-L-tryptophan;1H-Indole-3-propanoic acid, α-(1,3-dihydro-1,3-dioxo-2H-isoindol-2-yl)-, (αS)-;N-Phthaloyl-L-tryptophan (S)-3-(Indol-3-yl)-2-(1,3-dihydro-1,3-dioxo-2H-isoindol-2-yl)propanoic acid;CS-1518;DNA Methyltransferase Inhibitor
相关类别:
抑制剂;小分子抑制剂;细胞生物学试剂;表观遗传学;小分子抑制剂，天然产物;Inhibitors;DNA Methyltransferase Inhibitor;Epigenetics
沸点
606.0±50.0 °C(Predicted)
密度
1.502±0.06 g/cm3(Predicted)
酸度系数(pKa)
3.62±0.10(Predicted)
生物活性
RG108是一种DNA甲基转移酶抑制剂，IC50为115 nM，不会引起共价酶的诱捕。
体外研究
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. In another study, the synthesis and in vitro analysis of a biotinylated RG108 conjugate is investigated to evaluate the interactions with DNA methyltransferase enzymes. 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.
生物活性
RG108 (N-Phthalyl-L-tryptophan)是一种DNA methyltransferase抑制剂，无细胞试验中IC50为115 nM，不会引起共价酶的诱捕。
靶点
Target Value
DNA methyltransferase
(Cell-free assay) 115 nM
DNA methyltransferase
(Cell-free assay)
115 nM
体外研究
RG108有效阻断体外人细胞系中DNA甲基转移酶，并且不会引起共价酶俘获。细胞用低微摩尔浓度的RG108培育，导致基因组DNA显著脱甲基化，而没有可检测的毒性。有趣的是，RG108引起肿瘤抑制基因脱甲基和再活化，但是它不影响着丝粒基因序列的甲基化。在另一个研究中，进行生物素化RG108缀合物的合成和体外分析以评估与DNA甲基转移酶的相互作用。最近的研究表明，与天然SMs相比，RG108能够显著降低SM衍生的iPS细胞中DNA活性。
