3-({1-Hydroxy-1-[(N-{1-hydroxy-2-[(1-hydroxyethylidene)amino]-3-(4-hydroxyphenyl)propylidene}valyl)imino]propan-2-yl}amino)-4-oxobutanoic acid

개요Ac-YVAD-CHO is an inhibitor of caspase-1/interleukin-1β converting enzyme (ICE; Ki = 0.76 nM) and an acetylated form of the caspase-1 inhibitor YVAD-CHO . It is 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). It inhibits activation of caspase-1 and IL-1β in a cell-free assay using LPS-treated THP-1 cell homogenates when used at a concentration of 5 μM. Ac-YVAD-CHO (12.5 μmol/kg) 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 but does not decrease pancreatic expression of NOD-like receptor protein 3 (NLRP3). It increases susceptibility to lethal E. coli infection but prevents LPS-induced death in C3H/HeN mice when administered at doses of 5 and 10 mg/kg, respectively.

용도A potent, specific, and reversible inhibitor of caspases-1, -4 and -5