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RG108 N-Phthalyl-L-tryptophan

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。

  • 货号:
    TK0230
  • 规格:
    1mg
    5mg
    10mg
    50mg
  • 价格:
    0.00

产品参数

CAS No.48208-26-0
生物活性RG108 (N-Phthalyl-L-tryptophan) is a non-nucleoside DNA methyltransferases (DNMTs) inhibitor (IC50=115 nM) that blocks the DNMTs active site. RG108 (N-Phthalyl-L-tryptophan) causes demethylation and reactivation of tumor suppressor genes, but it does not affect the methylation of centromeric satellite sequences.
分子式C19H14N2O4
分子量334.33
运输条件Room temperature in continental US; may vary elsewhere.
储存条件Powder -20℃ 3 years
溶解性数据DMSO : 100 mg/mL (299.11 mM; Need ultrasonic) H2O : < 0.1 mg/mL (insoluble)
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.
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纯度及产品资料98%