R8279
RG108
≥98% (HPLC), powder
Synonyme(s) :
N-Phthalyl-L-tryptophan
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About This Item
Formule empirique (notation de Hill):
C19H14N2O4
Numéro CAS:
Poids moléculaire :
334.33
Code UNSPSC :
12352200
ID de substance PubChem :
Nomenclature NACRES :
NA.77
Produits recommandés
Niveau de qualité
Pureté
≥98% (HPLC)
Forme
powder
Activité optique
[α]/D -250 to -310°, c = 0.5 in methanol
Couleur
yellow
Solubilité
DMSO: >10 mg/mL
Température de stockage
−20°C
Chaîne SMILES
OC(=O)[C@H](Cc1c[nH]c2ccccc12)N3C(=O)C4=CCCC=C4C3=O
InChI
1S/C19H16N2O4/c22-17-13-6-1-2-7-14(13)18(23)21(17)16(19(24)25)9-11-10-20-15-8-4-3-5-12(11)15/h3-8,10,16,20H,1-2,9H2,(H,24,25)/t16-/m0/s1
Clé InChI
LMAZUAXDZRILNJ-INIZCTEOSA-N
Description générale
RG108, a non-nucleoside analog is also called [2-(1,3-dioxoisoindolin-2-yl)-3-(1H-indol-3-yl) propanoic acid.
Application
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)
Actions biochimiques/physiologiques
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.
RG108 is less cytotoxic compared to azacytidine (5-Aza-dCR). It mediates radiosensitivity in esophageal cancer cells (EC). RG108 is a potent epigenetic modulator and a demethylating agent. It elicits non-cytotoxic functionality and may be useful in stem cell therapies based on human bone marrow-derived mesenchymal stem cells (hBMSCs). It interacts with DNA methyltransferase 1 at the catalytic domain region.
Caractéristiques et avantages
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Code de la classe de stockage
11 - Combustible Solids
Classe de danger pour l'eau (WGK)
WGK 3
Point d'éclair (°F)
Not applicable
Point d'éclair (°C)
Not applicable
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Xiong Liu et al.
Cellular signalling, 51, 243-256 (2018-08-20)
It is well known that epithelial-mesenchymal transition (EMT) can confer cancer cells with invasive and migratory capabilities associated with distant metastasis. As a key upstream factor in the Hippo pathway, Kibra (wwc1 gene) has been shown to suppress EMT in
Stephanie Bridgeman et al.
Cancers, 11(4) (2019-04-13)
The potential anticancer effects of statins-a widely used class of cholesterol lowering drugs-has generated significant interest, as has the use of epigenetic modifying drugs such as HDAC and DNMT inhibitors. We set out to investigate the effect of statin drugs
Lucia Bialesova et al.
Scientific reports, 7(1), 10152-10152 (2017-09-02)
Increased adipocyte lipolysis links obesity to insulin resistance. The lipid droplet coating-protein Perilipin participates in regulation of lipolysis and is implicated in obesity. In the present study we investigate epigenetic regulation of the PLIN1 gene by correlating PLIN1 CpG methylation
German Todorov et al.
Scientific reports, 9(1), 8741-8741 (2019-06-21)
Mental health disorders are manifested in families, yet cannot be fully explained by classical Mendelian genetics. Changes in gene expression via epigenetics present a plausible mechanism. Anxiety often leads to avoidant behaviors which upon repetition may become habitual, maladaptive and
Peter Karagiannis et al.
Physiological reviews, 99(1), 79-114 (2018-10-18)
The discovery of somatic cell nuclear transfer proved that somatic cells can carry the same genetic code as the zygote, and that activating parts of this code are sufficient to reprogram the cell to an early developmental state. The discovery
Notre équipe de scientifiques dispose d'une expérience dans tous les secteurs de la recherche, notamment en sciences de la vie, science des matériaux, synthèse chimique, chromatographie, analyse et dans de nombreux autres domaines..
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