Irreversible, potent and selective cathepsin S inhibitor in vitro and in vivo.
LHVS is an irreversible, potent and selective cathepsin S inhibitor (CatS Ki = 5.9 nM; CatO2/L/B Ki = 0.23/0.72/39 μM, Cruzain Ki = 0.22 μM) that targets CatS active site thiol for covalent modification via its vinyl sulfone moiety. LHVS is a useful tool for studyting CatS-mediated responses in cultures (typical dosing ranges: 25 nM to 10μM) and in animals in vivo, including CatS-induced itch in mice (30 mg/kg sc.), morphine-induced antinociceptive tolerance in rats (50 nmol/rat itrathetically) and mechanical hyperalgesia in nerve-injured rats (3-30 mg/kg sc.).