RG108

Bezeichnung:RG108

CAS-Nr48208-26-0

Englisch Name:RG108

CBNumberCB0972112

SummenformelC19H14N2O4

Molgewicht334.33

MOL-Datei48208-26-0.mol

RG108 physikalisch-chemischer Eigenschaften

Schmelzpunkt	192-194℃
Siedepunkt	606.0±50.0 °C(Predicted)
Dichte	1.502±0.06 g/cm3(Predicted)
storage temp.	-20°C
Löslichkeit	DMSO: >10mg/mL
pka	3.62±0.10(Predicted)
Aggregatzustand	powder
Farbe	yellow
Sensitive	Light Sensitive
Stabilität	Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 1 month.
CAS Datenbank	48208-26-0

Sicherheit

WGK Germany	3
HS Code	2933.99.9701

RG108 Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
RG-108 (48208-26-0) is a non-nucleoside DNA methyltransferase inhibitor. IC50=115 nM1 Inhibits DNA methylation in human tumor cell lines without toxicity2. RG-108 enhances the reversion of neural progenitor cells to the pluripotent state.3
Verwenden
DNA methylation regulates gene expression in normal and malignant cells. RG-108 is a non-nucleoside DNA methyltransferase inhibitor (IC50 = 115 nM in vitro). It significantly reduces the methylation of genomic DNA in cells at 10 μM without detectable toxicity, distinguishing it from nucleoside-based inhibitors like 5-azacytidine. Further, RG-108 inhibits DNA methyltransferase activity by blocking the enzyme active site. Through these actions, RG-108 demethylates and reactivates epigenetically silenced tumor suppressor genes.
Verwenden
RG108 has been used:
- in reprogramming and increasing cell plasticity of primary multipotent mesenchymal stromal cells (MMSC)
- as an inhibitor of DNA methyltransferase (DNMTi) in human retinal pigment epithelial ARPE-19 cells
- as a DNA methyltransferase inhibitor in C33A2 cells to test its effect on papillomavirus late gene expression (HPV16)
Definition
ChEBI: (2S)-2-(1,3-dioxo-2-isoindolyl)-3-(1H-indol-3-yl)propanoic acid is an indolyl carboxylic acid.
Allgemeine Beschreibung
RG108, a non-nucleoside analog is also called [2-(1,3-dioxoisoindolin-2-yl)-3-(1H-indol-3-yl) propanoic acid.
Biologische Aktivität
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.
Biochem/physiol Actions
RG108 is a DNA methyltransferase (DMNT) inhibitor. It reactivates tumor suppressor gene expression (p16, SFRP1, secreted frizzled related protein-1, and TIMP-3) in tumor cells by DNA demethylation. RG108 also inhibits human tumor cell line (HCT116, NALM-6) proliferation and increased doubling time in culture.
Lager
Room temperature
Einzelnachweise
1) Brueckner et al. (2005), Epigenetic reactivation of tumor suppressor genes by a novel small-molecule inhibitor of human DNA methyltransferase; Cancer Res., 65 6305 2) Stresemann et al. (2006), Functional diversity of DNA methyltransferase inhibitors in human cancer cell lines; Cancer Res., 66 2794 3) Szablowska-Gadomska et al. (2012), Treatment with small molecules is an important milestone towards the induction of pluripotency in neural stem cells derived from human cord blood; Acta Neurobiol. Exp., 72 337

RG108 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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