L524-0366
Fn14 antagonist / 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 NFκB 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.
Biochemicals & reagents
951612-19-4
1) Dhruv et al. (2013), Structural basis and targeting of the interaction between fibroblast growth factor-inducible 14 and tumor necrosis factor-like weak inducer of apoptosis; J. Biol. Chem., 288 32261 2) Cheng et al. (2013), TWEAK/Fn14 Axis-Targeted Therapeutics: Moving Basic Science Discoveries to the Clinic; Front Immunol., 4 473
-20°C
PATHWAY: TNF; Autophagy; NFkappaB; Cell migration; Apoptosis inhibitor; Cytokine -- RESEARCH AREA: Cell death -- DISEASE AREA: Cancer; Inflammation