RG108 is a non-nucleoside DNA methyltransferase (DMNT) inhibitor. RG108 effectively blocked DNA methyltransferases in vitro and did not cause covalent enzyme trapping in human cell lines. RG108 also inhibits human tumor cell line (HCT116, NALM-6) proliferation and increased doubling time in culture. RG108 significantly reduces the methylation of genomic DNA in cells at 10 μM without detectable toxicity, distinguishing it from nucleoside-based inhibitors like 5-azacytidine. Through these actions, RG108 demethylates and reactivates epigenetically silenced tumor suppressor genes.
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Source | Eur Rev Med Pharmacol Sci (2017). Figure 2. RG108 |
| Method | FACS analysis | |
| Cell Lines | Ishikawa Cell | |
| Concentrations | 5 μM, 10 μM, 20 μM, 40 μM | |
| Incubation Time | 72 h | |
| Results | The proportion of cells in G2/M phase was gradually increased with the time |
| Cell Experiment | |
|---|---|
| Cell lines | HCT116 (left) and NALM-6 cells |
| Preparation method | Cell culture. NALM-6 ( 25) and HCT116 ( 26) cells were cultured under standard conditions in RPMI 1640 and McCoy's 5a medium, respectively. To analyze the effect of DNA methyltransferase inhibitors, cells were cultivated in media supplemented with 5-azacytidine, RG108, or RG119, as indicated. Unless stated otherwise, cells were harvested after 96 hours for further analysis. For the determination of cellular growth and viability, cells were stained with trypan blue and counted using a standard counting grid. |
| Concentrations | 10 μmol/L |
| Incubation time | 5 days |
| Animal Experiment | |
|---|---|
| Animal models | rat model of post kainic acid-induced epilepsy |
| Formulation | saline |
| Dosages | 5mg/kg |
| Administration | ip |
| Molecular Weight | 334.33 |
| Formula | C19H14N2O4 |
| CAS Number | 48208-26-0 |
| Solubility (25°C) | DMSO 50 mg/mL Ethanol 30 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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