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Beschreibung

A triazolyl-thiomorpholinyl-methanone compound that competes against TWEAK C-terminal/extracellular TNF homology domain (THD) for Fn14 binding (KD = 7.12 microM). Shown to completely inhibit 100 ng/mL sTWEAK-stimulated migration of T98G glioma cells at 10 microM concentration and is more potent against sTWEAK- than TNF&alpha,-induced NF-&kappa,B activation (IC50 = 7.8 vs. 31.03 microM, respectively, in reporter assays) without any apparent cytotoxicity up to 50 microM and 72 h in T98G cultures., A triazolyl-thiomorpholinyl-methanone compound that acts as a fibroblast growth factor-inducible 14 (Fn14) antagonist via direct affinity interaction (KD = 7.12 microM) and competes against TNF-like Weak Inducer of Apoptosis (TWEAK) C-terminal/extracellular TNF homology domain (THD) for Fn14 binding (16.8% inhibition against 500 pg/mL sTWEAK, [Drug] = 25 microM). Shown to completely inhibit 100 ng/mL sTWEAK-stimulated migration of T98G glioma cells at 10 microM concentration and is more potent against sTWEAK- than TNF&alpha,-induced NF-&kappa,B activation (IC50 = 7.8 vs. 31.03 microM, respectively, in reporter assays using Fn14-NF-kB-Luc and NF-&kappa,B-Luc cells) without any apparent cytotoxicity up to 50 microM and 72 h in T98G cultures.