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Beschreibung

A cell-permeable, bis-pyridinylbenzylethanamine that disrupts Fbxo3-Fbxl2 interaction by targeting Fbxo3 C-terminal ApaG domain and effectively prevents SCF-Fbxo3-catalyzed Fbxl2 ubiquitination, resulting in upregulation of cellular Fbxl2 and thereby SCF-Fbxl2-catalyzed ubiquitination of TRAFs (TNF Receptor-Associated Factors). Effectively reduces cellular TRAFs in human macrophage U937, PBMC, and murine murine MLE cultures (16 to 18 h with 5 to 127 µ,M BC-1215), resulting in downregulation of TRAF-mediated cytokines production from LPS-stimulated human PBMC (2 µ,g/mL LPS, 25 µ,M BC-1215,16 h). Intraperitoneal injection in mice in vivo (100 µ,g/mouse) is shown to greatly prevent circulating proinflammatory cytokines increase post CLP (Cecal Ligation & Puncture) and substantially reduce the severity of cell infiltration in lung after intratracheal P. aeruginosa PA103 infection., A cell-permeable, bis-pyridinylbenzylethanamine that disrupts Fbxo3-Fbxl2 interaction and effectively prevents SCF-Fbxo3-catalyzed Fbxl2 ubiquitination, resulting in cellular Fbxl2 upregulation and thereby SCF-Fbxl2-catalyzed TRAFs (TNF Receptor-Associated Factors) ubiquitination. Effectively reduces cellular TRAFs (5 to 127 µ,M) and prevents TRAF-mediated cytokines production from LPS-stimulated human PBMC (25 µ,M). Shown to greatly prevent Cecal Ligation & Puncture-induced plasma cytokine elevation and substantially reduce the severity of lung inflammation post intratracheal P. aeruginosa infection in mice (100 µ,g/mouse, i.p.) in vivo.