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RG108

Cat. No. M2182
RG108 Structure
Synonym:

N-Phthalyl-L-tryptophan

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
5mg USD 46  USD46 In stock
10mg USD 62  USD62 In stock
50mg USD 240  USD240 In stock
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Quality Control
Biological Activity

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.

Customer Product Validations & Biological Datas
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
Protocol
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
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 334.33
Formula C19H14N2O4
CAS Number 48208-26-0
Purity 100.0%
Solubility DMSO 50 mg/mL
Ethanol 30 mg/mL
Storage at -20°C
References

[1] Schirrmacher E, et al. Bioconjug Chem. Synthesis and in vitro evaluation of biotinylated RG108: a high affinity compound for studying binding interactions with human DNA methyltransferases.

[2] Stresemann C, et al. Cancer Res. Functional diversity of DNA methyltransferase inhibitors in human cancer cell lines.

[3] Brueckner B, et al. Cancer Res. Epigenetic reactivation of tumor suppressor genes by a novel small-molecule inhibitor of human DNA methyltransferases.

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Keywords: RG108, N-Phthalyl-L-tryptophan supplier, DNA Methyltransferase, inhibitors

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