RG108
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产品名称:RG108CAS:48208-26-0别名：N-邻苯二甲酰基-L-色氨酸;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)丙酸英文名：RG108
- 熔点 192-194℃
- 储存条件 Store at RT
- 溶解度 DMSO: >10mg/mL
- 颜色yellow
- 敏感性 Light Sensitive
- CAS 数据库48208-26-0
- 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.
