| Bioactivity | 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]. | ||||||||||||
| Invitro | LHVS (5 μM, 2 h) results in a 50% reduction of actin ring formation in wild-type osteoclasts when compared with untreated osteoclasts[1].LHVS acts in a dose-dependent manner on osteoclasts and at 5 μM, LHVS inhibits cathepsins K, L, S, and B[1].LHVS (1-5 nM) can inhibit specifically cathepsin S in HOM2 cells, leaving other cysteine proteases functionally active[3].LHVS impairs tachyzoite attachment by blocking the release of at least two key invasion proteins, MIC2 and M2AP, from the micronemes[2].LHVS (50 μM) selectively impairs microneme protein secretion[2]. | ||||||||||||
| In Vivo | LHVS (3-30 mg/kg, SC, once) shows anti-hyperalgesic effect in neuropathic rats[4].LHVS (30 nmol per rat, spinal delivery, daily) is antinociceptive in neuropathic rats[5].LHVS (1-50 nmol per rat, Intrathecal injection, daily) reverses established neuropathic mechanical hyperalgesia in 14-day neuropathic rats[5]. Animal Model: | ||||||||||||
| Name | LHVS | ||||||||||||
| CAS | 170111-28-1 | ||||||||||||
| Formula | C28H37N3O5S | ||||||||||||
| Molar Mass | 527.68 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. [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. [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. [4]. Barclay J, et al. Role of the cysteine protease cathepsin S in neuropathic hyperalgesia. Pain. 2007 Aug;130(3):225-234. [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. |