RG108

DNA methylation regulates gene expression in normal and malignant cells. RG108 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, RG108 inhibits DNA methyltransferase activity by blocking the enzyme active site. Through these actions, RG108 demethylates and reactivates epigenetically silenced tumor suppressor genes.Formal Name: alphaS-(1,3-dihydro-1,3-dioxo-2H-isoindol-2-yl)-1H-indole-3-propanoic acid. CAS Number: 48208-26-0. Synonyms: N-Phthalyl-L-Tryptophan. Molecular Formula: C19H14N2O4. Formula Weight: 334.3. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, Ethanol: 50 mg/ml, Ethanol:PBS (pH 7.2) (1:10): 0.1 mg/ml. lambdamax: 220, 283 nm. SMILES: O=C1N([C@H](C(O)=O)CC2=CNC3=C2C=CC=C3)C(C4=C1C=CC=C4)=O. InChi Code: InChI=1S/C19H14N2O4/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/h1-8,10,16,20H,9H2,(H,24,25). InChi Key: HPTXLHAHLXOAKV-UHFFFAOYSA-N.