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.
|Storage||Store at RT|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
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|
The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.
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
If you know of a relevant reference for RG 108, please let us know.
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Keywords: Non-nucleoside DNA methyltransferase inhibitor inhibitors transferases RG108 inhibits DNA methylation dnmt epigenetics DNA Methyltransferases
2 Citations for RG 108
Citations are publications that use Tocris products. Selected citations for RG 108 include:
Zhang et al (2016) Pharmacological reprogramming of fibroblasts into neural stem cells by signaling-directed transcriptional activation. Cell Stem Cell 18 653 PMID: 27133794
Nugent et al (2015) Brain feminization requires active repression of masculinization via DNA methylation. PLoS One 18 690 PMID: 25821913
Do you know of a great paper that uses RG 108 from Tocris? If so please let us know.
Literature in this Area
Epigenetics Scientific Review
Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.
Epigenetics Research Bulletin
Produced by Tocris and updated in 2014, the epigenetics research bulletin gives an introduction into mechanisms of epigenetic regulation, and highlights key Tocris products for epigenetics targets including:
- DNA Methyltransferases
- Histone Deacetylases
- Histone Demethylases
- Histone Methyltransferases