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Leupeptin Hemisulfate

Catalog No. T6564 CAS 103476-89-7

Leupeptin hemisulfate is a protease inhibitor with cell membrane-permeable, reversible, competitive, and oral activities. Leupeptin hemisulfate inhibits the activity of Cathepsin B, Cathepsin H, and Cathepsin L, and blocks fusion of amphipathic lysosomes. Leupeptin hemisulfate also has anti-inflammatory activity.

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Leupeptin Hemisulfate Chemical Structure

Leupeptin Hemisulfate, CAS 103476-89-7

Pack Size	Availability	Price/USD
5 mg	In stock	$ 47.00
10 mg	In stock	$ 67.00
25 mg	In stock	$ 112.00
50 mg	In stock	$ 166.00
100 mg	In stock	$ 246.00
1 mL * 10 mM (in DMSO)	In stock	$ 55.00

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Purity: 98.00%

Purity: 98%

Purity: 98.00%

Purity: 90%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Leupeptin hemisulfate is a protease inhibitor with cell membrane-permeable, reversible, competitive, and oral activities. Leupeptin hemisulfate inhibits the activity of Cathepsin B, Cathepsin H, and Cathepsin L, and blocks fusion of amphipathic lysosomes. Leupeptin hemisulfate also has anti-inflammatory activity.
In vitro	METHODS: SARS-CoV-2 infected Vero cells were treated with Leupeptin hemisulfate (0.06-200 µM) for 72 h, and the viral RNA level was detected by RT-PCR. RESULTS: Leupeptin hemisulfate inhibited SARS-CoV-2 RNA levels in Vero cells with an EC50 value of 42.34 µM. [1] METHODS: SARS-CoV-2 pseudovirus-infected Huh7 cells were treated with Leupeptin hemisulfate (0.1-100 µM) for 24 h. Pseudovirus infection was detected by luciferase activity assay. RESULTS: Leupeptin hemisulfate inhibited pseudovirus infection in Vero cells with an EC50 value of 39.29 µM. [2]
In vivo	METHODS: To determine macrophage autophagic flux, Leupeptin hemisulfate (9-40 mg/kg in 0.5 mL PBS) was administered to C57BL/6NCrl mice by single intraperitoneal injection. RESULTS: Leupeptin hemisulfate treatment resulted in the highest accumulation of LC3b in the liver and the lowest in the spleen. LC3a, ATG8/LC3b homologs, and the LC3b-interacting protein p62 were degraded with kinetics similar to those of LC3b. [3] METHODS: To examine whether cold activates autophagic flux, Leupeptin hemisulfate (40 mg/kg) was administered intraperitoneally to C57B6 mice in a single injection, and then the mice were cold-exposed at 4 ℃ for 1 h. The mice were then exposed to cold for 1 h. RESULTS: LC3-II flux in brown fat was increased >2-fold in cold-exposed mice. [4]
Kinase Assay	Determination of BET Protein Binding Affinities to I-BET726: For determination of binding affinities to BET protein bromodomains, I-BET726 is titrated against truncates containing both BD1 and BD2 of BRD2 (10 nM), BRD3 (10 nM), and BRD4 (10 nM) in 50 mM HEPES pH7.5, 150 mM NaCl, 5% Glycerol, 1 mM DTT and 1 mM CHAPS in the presence of an Alexa 647 derivative (50 nM) of fluorescent ligand. After equilibrating for 1 h, the bromodomain protein: ligand interaction is detected using Time Resolved Fluorescence Resonance Energy Transfer (TR-FRET) following the addition of 1.5 nM europium chelate labeled anti-6His antibody. Plates are read using an Envision Plate reader (λEX = 337 nm, λEM = 615 nm, λEM = 665 nm; dual dichroic = 400 nm & 630 nm). These data are fitted to a four parameter IC50 model using Graphit data analysis software.

Molecular Weight	475.59
Formula	C20H38N6O4·1/2H2SO4
CAS No.	103476-89-7

Storage

keep away from moisture

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: 87 mg/mL (182.9 mM)

DMSO: 88 mg/mL (185 mM)

Ethanol: 88 mg/mL (185 mM)

References and Literature

1. Fu L, et al. Mechanism of Microbial Metabolite Leupeptin in the Treatment of COVID-19 by Traditional Chinese Medicine Herbs. mBio. 2021 Oct 26;12(5):e0222021. 2. Yang WL, et al. Potential drug discovery for COVID-19 treatment targeting Cathepsin L using a deep learning-based strategy. Comput Struct Biotechnol J. 2022;20:2442-2454. 3. Haspel J, et al. Characterization of macroautophagic flux in vivo using a leupeptin-based assay. Autophagy. 2011 Jun;7(6):629-42. 4. Martinez-Lopez N, et al. Autophagy in the CNS and Periphery Coordinate Lipophagy and Lipolysis in the Brown Adipose Tissue and Liver. Cell Metab. 2016 Jan 12;23(1):113-27. 5. Jiang T Y, Pan Y F, Wan Z H, et al. PTEN status determines chemosensitivity to proteasome inhibition in cholangiocarcinoma[J]. Science Translational Medicine. 2020, 12(562).

Citations

1. Jiang T Y, Pan Y F, Wan Z H, et al. PTEN status determines chemosensitivity to proteasome inhibition in cholangiocarcinoma. Science Translational Medicine. 2020, 12(562). 2. Fu L, Shao S, Feng Y, et al. Mechanism of Microbial Metabolite Leupeptin in the Treatment of COVID-19 by Traditional Chinese Medicine Herbs. Mbio. 2021, 12(5): e02220-21. 3. Tao L, Cao Y, Wei Z, et al. Xanthatin triggers Chk1-mediated DNA damage response and destabilizes Cdc25C via lysosomal degradation in lung cancer cells. Toxicology and Applied Pharmacology. 2017 Dec 15;337:85-94 4. Tao L, Zhou K, Zhao Y, et al.Betulinic acid, a major therapeutic triterpene of Celastrus orbiculatus Thunb., acts as a chemosensitizer of gemcitabine by promoting Chk1 degradation.Journal of Ethnopharmacology.2023: 116295.

Related compound libraries

This product is contained In the following compound libraries：

Microbial Natural Product Library Peptide Compound Library Inhibitor Library Bioactive Compound Library NO PAINS Compound Library Protease Inhibitor Library Immunology/Inflammation Compound Library Anti-Tumor Natural Product Library Anti-Aging Compound Library Bioactive Compounds Library Max

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Keywords

Leupeptin Hemisulfate 103476-89-7 Proteases/Proteasome Serine Protease Cysteine Protease inhibit Cathepsin Inhibitor Leupeptin inhibitor

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