Description
L524-0366 (951612-19-4) is an 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. L524-0366 completely suppressed TWEAK-induced T98G cell migration (10 μM) without cytotoxicity up to 50 μM.1?L524-0366 is the first compound known to interfere with the TWEAK/Fn14 interaction and may serve as a lead compound for the development of new therapeutics.2
References
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
