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Leupeptin (hemisulfate)

Leupeptin hemisulfate is a broad-spectrum, membrane-permeable protease inhibitor. Leupeptin hemisulfate potently inhibits serine, cysteine and threonine proteases. Leupeptin hemisulfate inhibits Mpro (the main protease of SARS-CoV-2) and also has anti-inflammatory activity[1][2][3].

Product Specifications

CAS Number

[103476-89-7]

UNSPSC

12352211

Hazard Statement

H302, H315, H319, H335

Target

Cathepsin; Ser/Thr Protease; Virus Protease

Type

Natural Products

Related Pathways

Anti-infection; Metabolic Enzyme/Protease

Applications

COVID-19-immunoregulation

Field of Research

Infection; Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/Leupeptin-hemisulfate.html

Purity

99.39

Solubility

H2O : 70 mg/mL (ultrasonic)

Smiles

O=C[C@@H](NC([C@@H](NC([C@@H](NC(C)=O)CC(C)C)=O)CC(C)C)=O)CCCNC(N)=N.[0.5H2SO4]

Molecular Formula

C20H38N6O4.1/2H2SO4

Molecular Weight

475.59

Precautions

H302, H315, H319, H335

References & Citations

[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]Haspel J, et al. Characterization of macroautophagic flux in vivo using a leupeptin-based assay. Autophagy. 2011 Jun;7 (6) :629-42.|[3]Aoyagi T, et al. Biological activities of leupeptins. J Antibiot (Tokyo) . 1969 Nov;22 (11) :558-68.|[4]Aoyagi T, et al. Biological activities of leupeptins. J Antibiot (Tokyo) . 1969 Nov;22 (11) :558-68.

Shipping Conditions

Blue Ice

Storage Conditions

-20°C (Powder, sealed storage, away from moisture)

Scientific Category

Natural Products

Clinical Information

No Development Reported

Citation 01

Antiviral Res. 2020 Oct;182:104922.|Autophagy. 2021 Aug;17 (8) :1873-1888.|Autophagy. 2021 Jul;17 (7) :1592-1613.|Autophagy. 2024 Oct;20 (10) :2221-2237.|Autophagy. 2025 Aug 6:1-17.|Autophagy. 2025 Feb;21 (2) :352-373.|Biochem Pharmacol. 2022 Dec:206:115339.|Biochem Pharmacol. 2025 Apr 23:237:116955.|bioRxiv. 2020 Jun.|bioRxiv. 2023 Nov 5.|bioRxiv. 2024 November 14.|Br J Pharmacol. 2023 Aug;180 (15) :1930-1948.|Cancer Lett. 2022 Jun 1:535:215629.|Cell Death Differ. 2023 Jan;30 (1) :137-151.|Cell Death Dis. 2022 Oct 12;13 (10) :865.|Cell Rep. 2021 Nov 2;37 (5) :109931.|Complutense University of Madrid. 2025.|Environ Toxicol. 2024 Mar;39 (3) :1505-1520.|Int J Oncol. 2019 Jul;55 (1) :331-339.|J Biol Chem. 2021 Jan-Jun:296:100616.|J Clin Invest. 2022 Mar 1;132 (5) :e152170.|J Hematol Oncol. 2024 Sep 2;17 (1) :78.|J Inorg Biochem. 2025 Nov:272:113006.|mBio. 2024 Jun 28:e0053224.|Mol Biomed. 2023 Nov 17;4 (1) :42.|Nat Commun. 2025 Apr 2;16 (1) :3153.|Nat Commun. 2025 Jul 16;16 (1) :6551.|Nat Commun. 2025 Mar 11;16 (1) :2412.|Natl Sci Rev. 2021 Feb 10;8 (7) :nwab024.|Nature. 2024 Aug;632 (8025) :686-694.|Nature. 2024 Aug;632 (8026) :930-937.|Neuro Oncol. 2023 Jan 5;25 (1) :82-96.|Neurobiol Dis. 2025 Oct 15:215:107090.|Oncol Rep. 2021 Dec;46 (6) :253.|Pharmacol Res. 2024 Jun 28:107252.|Sci Adv. 2021 Jan 1;7 (1) :eabe1340.|Sci Rep. 2022 Jul 16;12 (1) :12197.|STAR Protoc. 2025 Jul 18;6 (3) :103963.|Structure. 2025 Sep 5.|Toxicol Appl Pharmacol. 2023 Jul 15:471:116568.|Adv Sci (Weinh) . 2025 Jul 15:e03486.|Biochem Biophys Res Commun. 2025 Apr 21:766:151870.|Biochem Pharmacol. 2024 Dec 19:116720.|Biochim Biophys Acta Mol Cell Res. 2023 Jan 24;1870 (3) :119433.|Carbohydr Polym. 2023 Oct 1:317:121108.|Cell Rep. 2025 Apr 2;44 (4) :115489.|Cell. 2025 Oct 24:S0092-8674 (25) 01131-6.|Chem Asian J. 2024 Sep 2:e202400824.|Emerg Microbes Infect. 2023 Dec;12 (1) :2207688.|Int J Biol Macromol. 2023 Aug 30:247:125670.|Nat Commun. 2025 Nov 19;16 (1) :10181.|Nature. 2023 Jun;618 (7966) :799-807.|Redox Biol. 2024 Apr:70:103064.|Redox Biol. 2024 May:71:103100.

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