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.
Synonyms: 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
Molecular Formula: C13H13ClN4OS
Molecular Weight: 308.79
Linear Structural Formula: C13H13ClN4OS
Purity: >=98% (HPLC)
Biochem Physiol Actions: Reversible: yes
Legal Information: CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Other Notes: Dhruv, H., et al. 2013. J. Biol. Chem.288, 32261.