RG108  48208-26-0

RG-108
分子式：C19H14N2O4   分子量：334.33
 
產(chǎn)品描述
RG108 是DNA methyltransferase抑制劑，IC50為115 nM。
靶點(diǎn)
DNA methyltransferase
         
IC50
115 nM
         
體外研究
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 salite 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.
體內(nèi)研究
 
溶解性
DMSO 67 mg/mL，水 <1 mg/mL，乙醇 67 mg/mL
穩(wěn)定性
2年 -20°C粉狀，6月-80°C溶于DMSO