Biological Activity
Non-nucleoside DNA methyltransferase inhibitor that blocks the enzyme active site. Inhibits DNA methylation in human cancer cell lines in vitro without detectable toxicity. Demethylates and reactivates epigenetically silenced tumor suppressor genes. Enhances the efficiency of induced pluripotent stem cell (iPS) generation.
Compound Libraries
RG 108 is also offered as part of the Tocriscreen Plus, Tocriscreen Epigenetics Toolbox and Tocriscreen Stem Cell Toolbox. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 334.33 |
| Formula | C19H14N2O4 |
| Storage | Store at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 48208-26-0 |
| PubChem ID | 702558 |
| InChI Key | HPTXLHAHLXOAKV-INIZCTEOSA-N |
| Smiles | O=C(C(C=CC=C4)=C4C3=O)N3[C@H](C(O)=O)CC2=CNC1=CC=CC=C12 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 33.43 | 100 | |
| ethanol | 33.43 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 334.33. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.99 mL | 14.96 mL | 29.91 mL |
| 5 mM | 0.6 mL | 2.99 mL | 5.98 mL |
| 10 mM | 0.3 mL | 1.5 mL | 2.99 mL |
| 50 mM | 0.06 mL | 0.3 mL | 0.6 mL |
Molarity Calculator
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Product Datasheets
References
References are publications that support the products' biological activity.
Brueckner et al (2005) Epigenetic reactivation of tumor suppressor genes by a novel small-molecule inhibitor of DNA methyltransferase. Cancer Res. 65 6305 PMID: 16024632
Stresemann et al (2006) Functional diversity of DNA methyltransferase inhibitors in human cancer cell lines. Cancer Res. 66 2794 PMID: 16510601
Schirrmacher et al (2006) Synthesis and in vitro evaluation of biotinylated RG108: a high affinity compound for studying binding interactions with human DNA methyltransferases. Bioconjug.Chem. 17 261 PMID: 16536454
Keywords: RG 108, supplier, Non-nucleoside, DNA, methyltransferase, inhibitor, inhibitors, transferases, RG108, inhibits, DNA, methylation, dnmt, epigenetics, DNA, Methyltransferases, Reprogramming, DNA, Methyltransferases, Tocris Bioscience
