R8279

RG108

≥98% (HPLC), powder

• Synonyme(s) : N-Phthalyl-L-tryptophan
• Formule empirique (notation de Hill) : C₁₉H₁₄N₂O₄
• CAS Number: 48208-26-0
• Poids moléculaire : 334.33
• Code UNSPSC : 12352200
• ID de substance PubChem : 24724594
• Nomenclature NACRES : NA.77

Propriétés

• Niveau de qualité: 100
• Essai: ≥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

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.

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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Informations sur la sécurité

• 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