Molecular Formula | C19H14N2O4
|
Molar Mass | 334.33 |
Density | 1.502±0.06 g/cm3(Predicted) |
Melting Point | 192-194℃ |
Boling Point | 606.0±50.0 °C(Predicted) |
Solubility | DMSO: >10mg/mL |
Appearance | powder |
Color | yellow |
pKa | 3.62±0.10(Predicted) |
Storage Condition | -20°C |
Stability | Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 1 month. |
Sensitive | Light Sensitive |
Use | RG108 is a DNA methyltransferase inhibitor, IC50 is 115 nM, and does not cause covalent enzyme trapping. |
In vitro study | RG108 potently blocks DNA methyltransferases in human cell lines in vitro and does not cause covalent enzyme entrapment. Incubation of cells with low micromolar concentrations of RG108 resulted in significant demethylation of genomic DNA without detectable toxicity. Interestingly, RG108 caused demethylation and reactivation of tumor suppressor genes, but it did not affect the methylation of centromeric gene sequences. In another study, synthesis and in vitro analysis of biotinylated RG108 conjugates were performed to assess interaction with DNA methyltransferases. Recent studies have shown that RG108 is able to significantly reduce DNA activity in SM-derived iPS cells compared to native SMs. |