RG 108
Chemical Name: N-Phthalyl-L-tryptophan
Purity: ≥99%
Biological Activity
RG 108 is a 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.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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Differences in the Epigenetic Regulation of Cytochrome P450 Genes between Human Embryonic Stem Cell-Derived Hepatocytes and Primary Hepatocytes.
Park H, Choi Y, Kim J, Chun H, Im I, Yoon S, Han Y, Song C, Kim H
PLoS ONE, 2015;10(7):e0132992. -
Epigenetic reactivation of tumor suppressor genes by a novel small-molecule inhibitor of DNA methyltransferase.
Brueckner et al.
Cancer Res., 2005;65:6305 -
Functional diversity of DNA methyltransferase inhibitors in human cancer cell lines.
Stresemann et al.
Cancer Res., 2006;66:2794 -
Synthesis and in vitro evaluation of biotinylated RG108: a high affinity compound for studying binding interactions with human DNA methyltransferases.
Schirrmacher et al.
Bioconjug.Chem., 2006;17:261
Product Datasheets
Citations for RG 108
The citations listed below are publications that use Tocris products. Selected citations for RG 108 include:
3 Citations: Showing 1 - 3
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LKB1 loss links serine metabolism to DNA methylation and tumorigenesis.
Authors: Kottakis Et al.
Nature 2016;539:390
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Pharmacological reprogramming of fibroblasts into neural stem cells by signaling-directed transcriptional activation.
Authors: Zhang Et al.
Cell Stem Cell 2016;18:653
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Brain feminization requires active repression of masculinization via DNA methylation.
Authors: Nugent Et al.
PLoS One 2015;18:690
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