Description
An inhibitor of caspase-1 (Ki = 0.76 nM); selective for caspase-1 over caspase-4, -5, -8, -9, and -10 (Kis = 163-970 nM), as well as over caspase-2, -3, -6, and -7 (Kis = >10,000 nM for all); inhibits activation of caspase-1 and IL-1β in a cell-free assay at 5 µM; reduces pancreatic levels of IL-18 and serum levels of IL-1β, as well as reduces pyroptosis of pancreatic cells, in a mouse model of cerulein-induced acute pancreatitis at 12.5 µmol/kg; increases susceptibility to lethal E. coli infection but prevents LPS-induced death in C3H-HeN mice at 5 and 10 mg/kg, respectively