170111-28-1

LHVS is a potent, non-selective, irreversible, cell-permeable cysteine protease and cathepsin inhibitor. LHVS decreases actin ring formation. LHVS inhibits T. gondii invasion with an IC50 of 10 μM[1][2][3].

LHVS is an irreversiblepotent and selective cathepsin S inhibitor (CatS Ki = 5.9 nM; CatO2/L/B Ki = 0.23/0.72/39 μMCruzain Ki = 0.22 μM) th at 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 vivoincluding CatS-induced itch in mice (30 mg/kg sc.)morphine-induced antinociceptive tolerance in rats (50 nmol/r at itrathetically) and mechanical hyperalgesia in nerve-injured rats (3-30 mg/kg sc.).

cathepsin S; cathepsin K; cathepsin L; Cathepsin B

Store at -20°C

[1] Wilson SR, et al. Cathepsin K activity-dependent regulation of osteoclast actin ring formation and bone resorption. J Biol Chem. 2009 Jan 23;284(4):2584-92. DOI:10.1074/jbc.M805280200
[2] Teo CF, et al.Cysteine protease inhibitors block Toxoplasma gondii microneme secretion and cell invasion. Antimicrob Agents Chemother. 2007 Feb;51(2):679-88. DOI:10.1128/AAC.01059-06
[3] Riese RJ, et al. Essential role for cathepsin S in MHC class II-associated invariant chain processing and peptide loading. Immunity. 1996 Apr;4(4):357-66. DOI:10.1016/s1074-7613(00)80249-6
[4] Barclay J, et al. Role of the cysteine protease cathepsin S in neuropathic hyperalgesia. Pain. 2007 Aug;130(3):225-234. DOI:10.1016/j.pain.2006.11.017
[5] Clark AK, et al. Inhibition of spinal microglial cathepsin S for the reversal of neuropathic pain. Proc Natl Acad Sci U S A. 2007 Jun 19;104(25):10655-60. DOI:10.1073/pnas.0610811104