RG108

DESCRIPTION

RG108 is a non-nucleoside DNA methyltransferase inhibitor by binding and blocking the active site of the methyltransferase enzyme. Unlike nucleoside based inhibitors, it reduces the methylation of DNA without detectable toxicity. RG108 is reported to be used to reactivate epigenetically silenced tumor suppressor genes and enhance the reprogramming efficiency of induced pluripotent stem cells.

DETAILS

Purity: ≥98%
Synonyms: RG-108, RG 108, CHEMBL1564869, NCI401077
Cas Number: 48208-26-0
References: Schirrmacher, E., Beck, C., Brueckner, B., Schmitges, F., Siedlecki, P., Bartenstein, P., ... & Schirrmacher, R. (2006). Synthesis and in vitro evaluation of biotinylated RG108: a high affinity compound for studying binding interactions with human DNA methyltransferases. Bioconjugate chemistry,17(2), 261-266. Asgatay, S., Champion, C., Marloie, G., Drujon, T., Senamaud-Beaufort, C., Ceccaldi, A., ... & Guianvarc’h, D. (2014). Synthesis and evaluation of analogues of N-phthaloyl-l-tryptophan (RG108) as inhibitors of DNA methyltransferase 1. Journal of medicinal chemistry, 57(2), 421-434. Shi, Y., Desponts, C., Do, J. T., Hahm, H. S., Schöler, H. R., & Ding, S. (2008). Induction of pluripotent stem cells from mouse embryonic fibroblasts by Oct4 and Klf4 with small-molecule compounds. Cell stem cell, 3(5), 568-574.
Application: FA
Formulation: Crystalline solid
Chemical Name: (2S)-2-(1,3-dioxoisoindol-2-yl)-3-(1H-indol-3-yl)propanoic acid
Molecular Weight: 334.3
Molecular Formula: C19H14N2O4
Storage Conditions: Product should be kept at -20°C.
Pubchem Openeye Can Smiles: C1=CC=C2C(=C1)C(=O)N(C2=O)C(CC3=CNC4=CC=CC=C43)C(=O)O