Fbxo3 Inhibitor, BC-1215

Cell permeable: yes

Primary Target
Fbox3

Reversible: yes

Toxicity: Standard Handling (A)

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 µM BC-1215), resulting in downregulation of TRAF-mediated cytokines production from LPS-stimulated human PBMC (2 µg/mL LPS; 25 µM BC-1215;16 h). Intraperitoneal injection in mice in vivo (100 µg/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.

Chen, B.B., et al. 2013. Nat. Immunol.14, 470.

Packaged under inert gas

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany