E3连接酶配体;E3 ligase Ligand;;InformationBC-1215 is an inhibitor of F-box protein 3 (Fbxo3, a ubiquitin E3 ligase component) with IC50 of 0.9 μg/mL and LC50 of 87 μg/ml for IL-1β release. BC-1215 inhibits the Fbxo3-TRAF activation pathway by destabilizing TRAF1-6.TargetsIL-1β release (Cell-free assay); IL-1β release (Cell-free assay) 0.9 μg/mL; 87 μg/mL(LC50)
体内研究:
BC-1215 (腹腔注射;100 μg) 减少细菌引起的炎症。
参考文献:
1. Chen BB, et al. A combinatorial F box protein directed pathway controls TRAF adaptor stability to regulateinflammation. Nat Immunol. 2013 May;14(5):470-9.