RG 108

Pricing Availability Delivery Time Qty
Cat.No. 3295 - RG 108 | C19H14N2O4 | CAS No. 48208-26-0
Description: Non-nucleoside DNA methyltransferase inhibitor
Chemical Name: N-Phthalyl-L-tryptophan
Purity: ≥99% (HPLC)
Datasheet
Citations (2)
Literature

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.

Select a batch to recalculate based on the batch molecular weight:
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

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Reconstitution Calculator

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

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


If you know of a relevant reference for RG 108, please let us know.

View Related Products by Product Action

View all DNA Methyltransferase Inhibitors

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.

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Reviews

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Literature in this Area

Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Epigenetics

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

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:

  • Bromodomains
  • DNA Methyltransferases
  • Histone Deacetylases
  • Histone Demethylases
  • Histone Methyltransferases

Pathways for RG 108

Protocols

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