Background
The peptide sulfate salt Leupeptin Hemisulfate is a serine and cysteine proteinase inhibitor that strongly blocks proteolysis by plasmin, trypsin, cathepsin B, and papain, but does not inhibit proteolysis by α-chymotrypsin or thrombin (1). Inhibition of the calcium-dependent protease calpain by Leupeptin Hemisulfate in murine cochlea explant cultures prevented hearing loss from aminoglycoside ototoxicity and neomycin-induced loss of outer hair cells (2). Leupeptin Hemisulfate inhibited calpain, rescued primary rat motoneurons exposed to α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) from cell death, and improved muscle function following nerve injury (3). Exposure of starved rats to Leupeptin Hemisulfate resulted in inhibition of lysosomal cysteine proteinases and blocked autolysosomal protein degradation, resulting in hepatic autolysosome accumulation (4). Leupeptin Hemisulfate is one of several inhibitors of cathepsin L, a cysteine protease that can cleave and activate the severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2) spike protein. Leupeptin Hemisulfate treatment of HuH-7 cells inhibited infection by live SARS-CoV-2 virus in vitro (5).
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- Momiyama, J. et al. (2006) Tohoku J Exp Med 209, 89-97.
- Kieran, D. and Greensmith, L. (2004) Neuroscience 125, 427-39.
- Ueno, T. and Komatsu, M. (2019) Methods Mol Biol 1880, 535-540.
- Yang, W.L. et al. (2022) Comput Struct Biotechnol J 20, 2442-2454.
Molecular Formula
C20H38N6O4 • 1/2H2SO4
Molecular Weight
475.6 g/mol
Purity
>96.5%
CAS
103476-89-7
Solubility
Soluble in methanol at 50 mg/mL or ethanol at 50 mg/mL or water at 50 mg/mL.
Storage
Directions for Use
Background References
Cross-Reactivity Key
H: human M: mouse R: rat Hm: hamster Mk: monkey Vir: virus Mi: mink C: chicken Dm: D. melanogaster X: Xenopus Z: zebrafish B: bovine Dg: dog Pg: pig Sc: S. cerevisiae Ce: C. elegans Hr: horse GP: Guinea Pig Rab: rabbit All: all species expected
Trademarks and Patents
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