RG-108
RG-108 is an inhibitor of DNA methyltransferases (DNMTs) that exhibits antidepressant, neuromodulatory, anticancer, and antiepileptic activities. RG-108 attenuates stress-induced behavioral adaptations in animal models and inhibits persistent epileptiform activity. RG-108 also increases TERT expression. In prostate cancer cells, this compound induces apoptosis and inhibits cell growth.
References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18958257
| Cas No. |
48208-26-0 |
|---|---|
| Formula |
C19H14N2O4 |
| Formula Wt. |
334.33 |
| IUPAC Name |
(2S)-2-(1,3-Dioxo-1,3-dihydro-2H-isoindol-2-yl)-3-(1H-indol-3-yl)propanoic acid |
Sales AJ, Joca SR. Effects of DNA methylation inhibitors and conventional antidepressants on mice behaviour and brain DNA methylation levels. Acta Neuropsychiatr. 2015 Jun 26:1-12. PMID: 26112212.
Oh YS, Jeong SG, Cho GW. Anti-senescence effects of DNA methyltransferase inhibitor RG108 in human bone marrow mesenchymal stromal cells. Biotechnol Appl Biochem. 2015 May 8. [Epub ahead of print]. PMID: 25952632.
Graça I, Sousa EJ, Baptista T, et al. Anti-tumoral effect of the non-nucleoside DNMT inhibitor RG108 in human prostate cancer cells. Curr Pharm Des. 2014;20(11):1803-11. PMID: 23888969.
Machnes ZM, Huang TC, Chang PK, et al. DNA methylation mediates persistent epileptiform activity in vitro and in vivo. PLoS One. 2013 Oct 2;8(10):e76299. PMID: 24098468.
