BC-1215

BC-1215 (BC1215) is a potent, highly unique, selective E3 ligase F box component Fbxo3 inhibitor with IL1β IC50 of 0.9 ug/mL; inhibits the Fbxo3-TRAF activation pathway for cytokine release, increases immunoreactive Fbxl2 levels and reduces TRAF proteins, impairs Fbxo3 ubiquitination of Fbxl2 with IC50 of 0.1 uM in vitro ubiquitination assay; reversibly inhibits Fbxo3 to destabilize TRAF proteins, remarkably suppresses the majority of the Th1 panel cytokines including G-CSF, GM-CSF, GROα, I-309, IL1-α, IL1-β, IL1rα, IL-6, IL-12, IL-23, MIP-1α, MIP-1β and TNFα, in PBMCs; ameliorates the severity of viral pneumonia, septic shock, colitis, and cytokine-driven inflammation systemically in murine models.Solid Tumors Phase 1 Clinical.