Date published: 2025-10-5

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RG 108 (CAS 48208-26-0)

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Alternate Names:
DNA Methyltransferase Inhibitor
Application:
RG 108 is a Dnmt inhibitor that silences tumor suppressor genes
CAS Number:
48208-26-0
Purity:
≥97%
Molecular Weight:
334.33
Molecular Formula:
C19H14N2O4
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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RG 108 is a non-nucleoside DNA methyltransferase (Dnmt) inhibitor that blocks the enzyme active site. RG 108 inhibits DNA methylation in human cancer cell lines without detectable toxicity in vitro. The compound demethylates and reactivates epigenetically silences tumor suppressor genes. RG 108 is a small molecule inhibitor that is used in the field of epigenetics and gene expression research. It specifically targets DNA methyltransferases (DNMTs), which are enzymes responsible for adding methyl groups to DNA molecules. By inhibiting DNMT activity, RG 108 can alter DNA methylation patterns and influence gene expression.


RG 108 (CAS 48208-26-0) References

  1. Sensitization by 5-azacytidine toward death receptor-induced hepatic apoptosis.  |  Weiland, T., et al. 2009. J Pharmacol Exp Ther. 328: 107-15. PMID: 18829727
  2. Epigenetic signatures in cancer: Implications for the control of cancer in the clinic.  |  Lima, SC., et al. 2010. Curr Opin Mol Ther. 12: 316-24. PMID: 20521220
  3. Tenuipyrone, a novel skeletal polyketide from the entomopathogenic fungus, Isaria tenuipes, cultivated in the presence of epigenetic modifiers.  |  Asai, T., et al. 2012. Org Lett. 14: 513-5. PMID: 22201477
  4. Treatment with small molecules is an important milestone towards the induction of pluripotency in neural stem cells derived from human cord blood.  |  Szablowska-Gadomska, I., et al. 2012. Acta Neurobiol Exp (Wars). 72: 337-50. PMID: 23377265
  5. Differential contributions of de novo and maintenance DNA methyltransferases to object memory processing in the rat hippocampus and perirhinal cortex--a double dissociation.  |  Mitchnick, KA., et al. 2015. Eur J Neurosci. 41: 773-86. PMID: 25639476
  6. Comparing The Effects of Small Molecules BIX-01294, Bay K8644, RG-108 and Valproic Acid, and Their Different Combinations on Induction of Pluripotency Marker-Genes by Oct4 in The Mouse Brain.  |  Asadi, S., et al. 2015. Cell J. 16: 416-25. PMID: 25685732
  7. Specific combinations of the chromatin-modifying enzyme modulators significantly attenuate glioblastoma cell proliferation and viability while exerting minimal effect on normal adult stem cells growth.  |  Alexanian, AR. and Huang, YW. 2015. Tumour Biol. 36: 9067-72. PMID: 26084611
  8. Pharmacokinetics of the Experimental Non-Nucleosidic DNA Methyl Transferase Inhibitor N-Phthalyl-L-Tryptophan (RG 108) in Rats.  |  Schneeberger, Y., et al. 2016. Basic Clin Pharmacol Toxicol. 118: 327-32. PMID: 26525153
  9. Activation of SIRT6 by DNA hypomethylating agents and clinical consequences on combination therapy in leukemia.  |  Carraway, HE., et al. 2020. Sci Rep. 10: 10325. PMID: 32587297
  10. Differentiation of mouse embryonic stem cells into cells with spermatogonia-like morphology with chemical intervention-dependent increased gene expression of LIM homeobox 1 (Lhx1).  |  Moshfegh, C., et al. 2022. Stem Cell Res. 61: 102780. PMID: 35395624
  11. Unique combinations of epigenetic modifiers synergistically impair the viability of the U87 glioblastoma cell line while exhibiting minor or moderate effects on normal stem cell growth.  |  Alexanian, AR. and Brannon, A. 2022. Med Oncol. 39: 86. PMID: 35478054
  12. Tissue-specific identification of multi-omics features for pan-cancer drug response prediction.  |  Zhao, Z., et al. 2022. iScience. 25: 104767. PMID: 35992090
  13. EnrichIntersect: an R package for custom set enrichment analysis and interactive visualization of intersecting sets.  |  Zhao, Z., et al. 2022. Bioinform Adv. 2: vbac073. PMID: 36699400

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

RG 108, 10 mg

sc-204235
10 mg
$128.00

RG 108, 50 mg

sc-204235A
50 mg
$505.00