BC-1215

BC-1215 is an inhibitor of F-box protein 3 (FBXO3; IC₅₀ = 0.9 μg/mL for Il-1β release).¹ It decreases FBXO3 interaction with F-box/LRR-repeat protein 2 (FBXL2) in a dose-dependent manner and prevents FBXO3-dependent ubiquitination of FBXL2. It also lowers expression of Tnf receptor-associated factors (TRAFs) 1-6 without affecting TRAF1-6 mRNA levels in resting and LPS-stimulated peripheral blood mononuclear cells (PBMCs). BC-1215 (100 μg, i.p., per animal) reduces plasma levels of the inflammatory cytokines Il-6, Tnf, and Il-1β and decreases peritoneal bacteria counts in a mouse model of cecal ligation and puncture-induced sepsis. It also reduces inflammation in mouse models of DSS-induced colitis, paw edema, and ear edema.²

WARNING This product is not for human or veterinary use.

1. Chen, B.B., Coon, T.A., Glasser, J.R., et al. A combinatorial F box protein directed pathway controls TRAF adaptor stability to regulate inflammation. Nat. Immunol. 14(5), 470-479 (2013).

2. Mallampalli, R.K., Coon, T.A., Glasser, J.R., et al. Targeting F box protein Fbxo3 to control cytokine-driven inflammation. J. Immunol. 191(10), 5247-5255 (2013).