Fn14 Antagonist, L524-0366 – Calbiochem

Descrição detalhada : 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 TNFα-induced NF-κB 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 TNFα-induced NF-κB activation (IC50 = 7.8 vs. 31.03 microM, respectively, in reporter assays using Fn14-NF-kB-Luc and NF-κB-Luc cells) without any apparent cytotoxicity up to 50 microM and 72 h in T98G cultures.
Sinónimos : Fn14 Antagonist, L524-0366 - Calbiochem; Fibroblast Growth Factor-inducible 14 Antagonist; L5240366, THD Receptor Antagonist; TNF-like Weak Inducer of Apoptosis Receptor Antagonist, TWEAK Receptor Antagonist; TWEAK-Fn14 Interaction Inhibitor
Fórmula molecula r: C13H13ClN4OS
Armazenamento : 2-8C; 2-8C
Embalagem : 1X1EA