product name Leupeptin Hemisulfate
Description: Leupeptin Hemisulfate is a reversible inhibitor of serine and cysteine proteases with Ki values of 35 nM, 3.4 μM, 6 nM and 72 nM for bovine trypsin, human plasmin, bovine spleen cathepsin B and recombinant human calpain, respectively. As a protease inhibitor, leupeptin was originally isolated from the Streptomyces species. It exerted poor membrane permeability due to its polar C-terminal.
References: J Antibiot (Tokyo). 1969 Nov;22(11):558-68; Cell Biol Int Rep. 1985 Sep;9(9):849-57.
475.59
Formula
C20H38N6O4.1/2H2SO4
CAS No.
103476-89-7
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 95 mg/mL (199.8 mM)
Water: 95 mg/mL (199.8 mM)
Ethanol: 95 mg/mL (199.8 mM)
Solubility (In vivo)
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19409785
| In Vitro |
In vitro activity: Leupeptin, produced by various species of actinomycetes, strongly inhibit proteolysis. Leupeptin hemisulfate protects tubulin from endogenous proteolytic activities during the isolation procedure and results in increased tubulin purity. Leupeptin hemisulfate could restore up to 50% of hepatitis B surface antigen (HBsAg) expression in cell suspension cultures. Kinase Assay: Cell Assay: In cultures of MRC-C cells, Leupeptin prevented multiplication of the human coronavirus strain 229E. The IC50 value of Leupeptin in plaque tests was 0.4 μg/mL, whilst growth of host cells was unaffected by Leupeptin at 50 μg/mL. In single-cycle growth experiments, Leupeptin (100 μg/mL) reduced virus yield only if added within 2 hrs of infection, indicating its action on an early stage of virus replication. |
|---|---|
| In Vivo | Leupeptin was well tolerated by the animals and dose-dependently produced a substantial increase in LC3b-II in both the total tissue extracts and the lysosome enriched fraction (LE fraction). At the electron microscopy (EM) level, leupeptin induced the accumulation of electron-dense vesicular structures that, in hepatocytes, were visible by 60 min after treatment (40 mg/kg). The results suggested that Leupeptin enhanced LC3b-II levels in vivo by protecting this protein from being degraded inside lysosomes, and thus the leupeptin-based assay could be potentially used for studying the dynamics of macroautophagy in mice. |
| Animal model | C57BL/6NCrl male mice |
| Formulation & Dosage | 0, 9, 18 36 and 40 mg/kg; i.p. injection |
| References | J Antibiot (Tokyo). 1969 Nov;22(11):558-68; Cell Biol Int Rep. 1985 Sep;9(9):849-57; Plant Cell Rep. 2007 Sep;26(9):1575-84. |
