UCB-9260

1515888-53-5

423.51

10 mM in DMSO

Apoptosis

UCB-9260, an orally active compound, inhibits TNF signalling by stabilising an asymmetric form of the trimer. UCB-9260 is selective for TNF over other superfamily members, and binds TNF with a similar K_d of 13?nM^[1]. In Vitro: UCB-9260 (0-10 uM) inhibits NF-kappaB with a geometric mean IC₅₀ of 202?nM after TNF (10?pM) stimulation in in Hek-293 cells^[1].
UCB-9260 inhibits TNF-dependent cytotoxicity with a geometric mean IC₅₀ of 116?nM and a geometric mean IC₅₀ of 120?nM, using human and mouse TNF, respectively^[1]. In Vivo: UCB-9260 (150?mg/kg; p.o.; twice daily for 7 days) shows a significant reduction of the clinical score^[1].
UCB-9260 (10-300?mg/kg; p.o.) dose-dependently inhibits human and mouse TNF-induced neutrophil recruitment to the peritoneal compartment in adult male Balb/c mice^[1].