Fn14 antagonist. Competes with TNF-like weak inducer of apoptosis (TWEAK) C-terminal/extracellular TNF homology domain (THD) for Fn14 binding (KD = 7.12 µM). It specifically inhibits TWEAK-Fn14-mediated NFkappaB activation. It completely suppressed TWEAK-induced T98G cell migration (10 µM) without cytotoxicity up to 50 µM1. L524-0366 is the first compound known to interfere with the TWEAK/Fn14 inter-action and may serve as a lead compound for the development of new therapeutics2.
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