Leupeptin
Based on 61 publication(s) in Google Scholar
Leupeptin is a broad-spectrum, membrane-permeable protease inhibitor. Leupeptin potently inhibits serine, cysteine and threonine proteases. Leupeptin inhibits Mpro (the main protease of SARS-CoV-2) and also has anti-inflammatory activity.
For research use only. We do not sell to patients.
- CAS No.: 55123-66-5
- Formula: C20H38N6O4
- Molecular Weight:426.55
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications Citing Use of MedChemExpress (MCE) Leupeptin
More- Signal Transduct Target Ther. 2025 Dec 15;10(1):406. [Abstract]
- Nature. 2024 Aug;632(8025):686-694. [Abstract]
- Nature. 2024 Aug;632(8026):930-937. [Abstract]
- Nature. 2023 Jun;618(7966):799-807. [Abstract]
- Cell. 2025 Nov 26;188(24):6861-6872.e14. [Abstract]
- Nat Biotechnol. 2025 Sep 10. [Abstract]
- J Hematol Oncol. 2024 Sep 2;17(1):78. [Abstract]
- Cell Res. 2025 May;35(5):385-388. [Abstract]
- Natl Sci Rev. 2021 Feb 10;8(7):nwab024. [Abstract]
- Nat Commun. 2025 Nov 19;16(1):10181. [Abstract]
- Nat Commun. 2025 Jul 16;16(1):6551. [Abstract]
- Nat Commun. 2025 Apr 2;16(1):3153. [Abstract]
- Nat Commun. 2025 Mar 11;16(1):2412. [Abstract]
- Nat Commun. 2019 Jan 24;10(1):411. [Abstract]
- Cell Death Differ. 2023 Jan;30(1):137-151. [Abstract]
- Autophagy. 2025 Aug 6:1-17. [Abstract]
- Autophagy. 2025 Feb;21(2):352-373. [Abstract]
- Autophagy. 2024 Oct;20(10):2221-2237. [Abstract]
- Autophagy. 2021 Aug;17(8):1873-1888. [Abstract]
- Autophagy. 2021 Jul;17(7):1592-1613. [Abstract]
- Adv Sci (Weinh). 2025 Jul 15:e03486. [Abstract]
- J Clin Invest. 2022 Mar 1;132(5):e152170. [Abstract]
- Neuro Oncol. 2023 Jan 5;25(1):82-96. [Abstract]
- Sci Adv. 2026 Jan 30;12(5):eadz8234. [Abstract]
- Carbohydr Polym. 2023 Oct 1:317:121108. [Abstract]
- Sci Adv. 2021 Jan 1;7(1):eabe1340. [Abstract]
- Metabolism. 2026 May:178:156553. [Abstract]
- Redox Biol. 2024 May:71:103100. [Abstract]
- Redox Biol. 2024 Apr:70:103064. [Abstract]
- Pharmacol Res. 2024 Jun 28:107252. [Abstract]
- Mol Biomed. 2023 Nov 17;4(1):42. [Abstract]
- Cancer Lett. 2022 Jun 1:535:215629. [Abstract]
- Cell Death Dis. 2022 Oct 12;13(10):865. [Abstract]
- Int J Biol Macromol. 2023 Aug 30:247:125670. [Abstract]
- Br J Pharmacol. 2023 Aug;180(15):1930-1948. [Abstract]
- Emerg Microbes Infect. 2023 Dec;12(1):2207688. [Abstract]
- Cell Rep. 2025 Apr 2;44(4):115489. [Abstract]
- Cell Rep. 2021 Nov 2;37(5):109931. [Abstract]
- Neurobiol Dis. 2025 Oct 15:215:107090. [Abstract]
- Biochem Pharmacol. 2025 Apr 23:237:116955. [Abstract]
- Biochem Pharmacol. 2024 Dec 19:116720. [Abstract]
- Biochem Pharmacol. 2022 Dec:206:115339. [Abstract]
- Int J Oncol. 2019 Jul;55(1):331-339. [Abstract]
- mBio. 2024 Jun 28:e0053224. [Abstract]
- Structure. 2025 Dec 4;33(12):2049-2057.e5. [Abstract]
- Antiviral Res. 2020 Oct;182:104922. [Abstract]
- Sci Rep. 2022 Jul 16;12(1):12197. [Abstract]
- Oncol Rep. 2021 Dec;46(6):253. [Abstract]
- J Biol Chem. 2021 Jan-Jun:296:100616. [Abstract]
- Biochim Biophys Acta Mol Cell Res. 2023 Jan 24;1870(3):119433. [Abstract]
- Toxicol Appl Pharmacol. 2023 Jul 15:471:116568. [Abstract]
- Chem Asian J. 2024 Sep 2:e202400824. [Abstract]
- J Inorg Biochem. 2025 Nov:272:113006. [Abstract]
- Environ Toxicol. 2024 Mar;39(3):1505-1520. [Abstract]
- Biochem Biophys Res Commun. 2025 Apr 21:766:151870. [Abstract]
- STAR Protoc. 2025 Jul 18;6(3):103963. [Abstract]
- bioRxiv. 2026 Jan 26:2026.01.23.701155. [Abstract]
- Complutense University of Madrid. 2025.
- bioRxiv. 2024 November 14.
- bioRxiv. 2023 Nov 5.
- bioRxiv. 2020 Jun.
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All Cathepsin Isoforms
More
Biological Activity
Cathepsin B, Cathepsin H, Cathepsin L, Ser/Thr Protease, Mpro[1][2][3].
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HeLa | IC50 |
>224 μM
Compound: 1
|
Antiviral activity against human rhinovirus-14 in HeLa cells
Antiviral activity against human rhinovirus-14 in HeLa cells
|
10.1016/S0960-894X(96)00537-9 |
Leupeptin (0.06-200 μM; 72 h) significantly decreases copy numbers of SARS-CoV-2 viral RNA (vRNA) in Vero cells[1]
Leupeptin inhibits RNA levels of SARS-CoV-2 in Vero cells, with an EC50 value of 42.34 μM[1].
Leupeptin has some inhibitory activity against Mpro, with an IC50 value of 127.2 μM[1].
Leupeptin againsts human coronavirus strain 229E with an IC50 value of 0.4 μg/mL (about 1 μM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Vero cells
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Concentration:0.06-200 µM
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Incubation Time:72 h
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Result:Significantly decreased copy numbers of SARS-CoV-2 viral RNA (vRNA).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6NCrl male mice (6-8 weeks old, 20-25 g)[1].
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Dosage:0, 9, 18, 36 mg/kg
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Administration:Intraperitoneal injection; single
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Result:Promoted the accumulation of LC3b-II in mouse liver.
Chemical Information
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CAS No. 55123-66-5
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Molecular Weight 426.55
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Formula C20H38N6O4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (61)
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Journal Impact Factor
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Most Recent
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Signal Transduct Target Ther
Selective depletion of tumor-associated SAMHD1 enhances chemotherapeutic efficacy and antitumor immune responses. [Abstract]2025 Dec 15;10(1):406. PMID: 41392286 -
Nature
2024 Aug;632(8025):686-694. PMID: 39112701 -
Nature
2024 Aug;632(8026):930-937. PMID: 39085602 -
Nature
2023 Jun;618(7966):799-807. PMID: 37316670 -
Cell
2025 Nov 26;188(24):6861-6872.e14. PMID: 41138730 -
Nat Biotechnol
A rapid imaging-based screen for induced-proximity degraders identifies a potent degrader of oncoprotein SKP2. [Abstract]2025 Sep 10. PMID: 40931108 -
J Hematol Oncol
METTL16-SENP3-LTF axis confers ferroptosis resistance and facilitates tumorigenesis in hepatocellular carcinoma. [Abstract]2024 Sep 2;17(1):78. PMID: 39218945
Leupeptin purchased from MedChemExpress. Usage Cited in: J Hematol Oncol. 2024 Sep 2;17(1):78. [Abstract]
The LTF expression was detected under MG132 (10 μM) or Leupeptin (100 μM) treatment.
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Cell Res
Structural basis of augmenting taurine uptake by the taurine transporter in alleviating cellular senescence. [Abstract]2025 May;35(5):385-388. PMID: 40108449 -
Natl Sci Rev
SNX14 deficiency-induced defective axonal mitochondrial transport in Purkinje cells underlies cerebellar ataxia and can be reversed by valproate. [Abstract]2021 Feb 10;8(7):nwab024. PMID: 34691693 -
Nat Commun
PRDX1 promotes testosterone synthesis and attenuates aging via redox regulation of ATG4B to modulate lipophagy. [Abstract]2025 Nov 19;16(1):10181. PMID: 41261096 -
Nat Commun
2025 Jul 16;16(1):6551. PMID: 40670375 -
Nat Commun
Molecular insights into the α6β4 nicotinic acetylcholine receptor function and ligand recognition. [Abstract]2025 Apr 2;16(1):3153. PMID: 40175361 -
Nat Commun
2025 Mar 11;16(1):2412. PMID: 40069141 -
Nat Commun
Usp7 regulates Hippo pathway through deubiquitinating the transcriptional coactivator Yorkie. [Abstract]2019 Jan 24;10(1):411. PMID: 30679505 -
Cell Death Differ
SOCS2-enhanced ubiquitination of SLC7A11 promotes ferroptosis and radiosensitization in hepatocellular carcinoma. [Abstract]2023 Jan;30(1):137-151. PMID: 35995846
Leupeptin purchased from MedChemExpress. Usage Cited in: Cell Death Differ. 2023 Jan;30(1):137-151. [Abstract]
Western blot analysis of SLC7A11, SOCS2 and tubulin proteins in SK-Hep-1 and HepG2 cells at 4 h after 4 Gy IR. Leupeptin (50 μM) were added before IR.
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Autophagy
Dysfunctional autophagy triggers STING1 activation to exacerbate cartilage degeneration in obesity-associated osteoarthritis. [Abstract]2025 Aug 6:1-17. PMID: 40728163 -
Autophagy
Impaired degradation of PLCG1 by chaperone-mediated autophagy promotes cellular senescence and intervertebral disc degeneration. [Abstract]2025 Feb;21(2):352-373. PMID: 39212196
Leupeptin purchased from MedChemExpress. Usage Cited in: Autophagy. 2025 Feb;21(2):352-373. [Abstract]
Immunoblotting showing the level of PLCG1 in NPC after treatment with Leu (10 μM), NH4Cl (20 mM), or their combination for 12 h. Right panels represent normalized (/NC) band intensities of interest.
Leupeptin purchased from MedChemExpress. Usage Cited in: Autophagy. 2025 Feb;21(2):352-373. [Abstract]
Western blot showing PLCG1 levels in NPC treated with a combination of Leu (10 μM) and NH4Cl (N/L) for 3, 6, and 9 h. Right panels represent normalized (/NC) band intensities of interest.
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Autophagy
PLK2-mediated phosphorylation of SQSTM1 S349 promotes aggregation of polyubiquitinated proteins upon proteasomal dysfunction. [Abstract]2024 Oct;20(10):2221-2237. PMID: 39316746 -
Autophagy
Mice deficient in UXT exhibit retinitis pigmentosa-like features via aberrant autophagy activation. [Abstract]2021 Aug;17(8):1873-1888. PMID: 32744119
Leupeptin purchased from MedChemExpress. Usage Cited in: Autophagy. 2021 Aug;17(8):1873-1888. [Abstract]
661 W cells were transfected with the indicated siRNA for 24 h. Then, 661 W cells were treated with 10 μg/ml Leupeptin for 24 h. Cell lysates were collected for western blot analysis of LC3B and GAPDH.
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Autophagy
Discovery of a potent SCAP degrader that ameliorates HFD-induced obesity, hyperlipidemia and insulin resistance via an autophagy-independent lysosomal pathway. [Abstract]2021 Jul;17(7):1592-1613. PMID: 32432943 -
Adv Sci (Weinh)
LncDARS-AS1 Regulates ATP1A1 Stability and Enhances Na+/K+ ATPase Activity to Promote Osteosarcoma Metastasis. [Abstract]2025 Jul 15:e03486. PMID: 40665639 -
J Clin Invest
USP25 inhibition ameliorates Alzheimer's pathology through the regulation of APP processing and Aβ generation. [Abstract]2022 Mar 1;132(5):e152170. PMID: 35229730 -
Neuro Oncol
2023 Jan 5;25(1):82-96. PMID: 35727735 -
Sci Adv
Structural insight into the glucose-6-phosphate transport by G6PT1 and inhibition mechanism of CGA. [Abstract]2026 Jan 30;12(5):eadz8234. PMID: 41616054 -
Carbohydr Polym
Metabolic degradation of polysaccharides from Lentinus edodes by Kupffer cells via the Dectin-1/Syk signaling pathway. [Abstract]2023 Oct 1:317:121108. PMID: 37364942 -
Sci Adv
Trisomy 21-induced dysregulation of microglial homeostasis in Alzheimer's brains is mediated by USP25. [Abstract]2021 Jan 1;7(1):eabe1340. PMID: 33523861 -
Metabolism
PFKFB3 nuclear translocation improves diabetic retinopathy by attenuating endothelial cell senescence through inhibition of USP7-p53 axis. [Abstract]2026 May:178:156553. PMID: 41655956 -
Redox Biol
IL-13 facilitates ferroptotic death in asthmatic epithelial cells via SOCS1-mediated ubiquitinated degradation of SLC7A11. [Abstract]2024 May:71:103100. PMID: 38484644 -
Redox Biol
SELENOK-dependent CD36 palmitoylation regulates microglial functions and Aβ phagocytosis. [Abstract]2024 Apr:70:103064. PMID: 38320455 -
Pharmacol Res
Cyclopeptide RA-V from Rubia yunnanensis restores activity of Adagrasib against colorectal cancer by reducing the expression of Nrf2. [Abstract]2024 Jun 28:107252. PMID: 38945380 -
Mol Biomed
Aloperine targets lysosomes to inhibit late autophagy and induces cell death through apoptosis and paraptosis in glioblastoma. [Abstract]2023 Nov 17;4(1):42. PMID: 37975957 -
Cancer Lett
Rab8A promotes breast cancer progression by increasing surface expression of Tropomyosin-related kinase B. [Abstract]2022 Jun 1:535:215629. PMID: 35278612 -
Cell Death Dis
Mesenchymal stem cells exosomal let-7a-5p improve autophagic flux and alleviate liver injury in acute-on-chronic liver failure by promoting nuclear expression of TFEB. [Abstract]2022 Oct 12;13(10):865. PMID: 36224178 -
Int J Biol Macromol
ADRM1/RPN13 attenuates cartilage extracellular matrix degradation via enhancing UCH37-mediated ALK5 deubiquitination. [Abstract]2023 Aug 30:247:125670. PMID: 37406898 -
Br J Pharmacol
A novel sorbicillinoid compound as a potent anti-inflammation agent through inducing NLRP3 protein degradation. [Abstract]2023 Aug;180(15):1930-1948. PMID: 36788033 -
Emerg Microbes Infect
Porcine deltacoronavirus resists antibody neutralization through cell-to-cell transmission. [Abstract]2023 Dec;12(1):2207688. PMID: 37125733 -
Cell Rep
LAMP2A-mediated neuronal hyperexcitability by enhancing NKAβ1 degradation underlies depression-induced allodynia. [Abstract]2025 Apr 2;44(4):115489. PMID: 40178973 -
Cell Rep
2021 Nov 2;37(5):109931. PMID: 34731621 -
Neurobiol Dis
2025 Oct 15:215:107090. PMID: 40930427 -
Biochem Pharmacol
GSNO induced mitochondrial Cx43 nitrosylation in cardiomyocyte differentiation from mouse ES cells in vitro. [Abstract]2025 Apr 23:237:116955. PMID: 40280246 -
Biochem Pharmacol
E3 ubiquitin ligase ITCH-mediated proteasomal degradation of WBP2 sensitizes breast cancer cells to chemotherapy through restraining AMOTL2/c-JUN axis. [Abstract]2024 Dec 19:116720. PMID: 39709035 -
Biochem Pharmacol
The ubiquitination of CKIP-1 mediated by Src aggravates diabetic renal fibrosis (original article). [Abstract]2022 Dec:206:115339. PMID: 36347273 -
Int J Oncol
Metformin induces TPC-1 cell apoptosis through endoplasmic reticulum stress-associated pathways in vitro and in vivo. [Abstract]2019 Jul;55(1):331-339. PMID: 31180536 -
mBio
PRRSV GP5 inhibits the antivirus effects of chaperone-mediated autophagy by targeting LAMP2A. [Abstract]2024 Jun 28:e0053224. PMID: 38940560 -
Structure
2025 Dec 4;33(12):2049-2057.e5. PMID: 40914153 -
Antiviral Res
ML-SA1, a selective TRPML agonist, inhibits DENV2 and ZIKV by promoting lysosomal acidification and protease activity. [Abstract]2020 Oct;182:104922. PMID: 32858116 -
Sci Rep
Hepatitis C virus NS3/4A inhibitors and other drug-like compounds as covalent binders of SARS-CoV-2 main protease. [Abstract]2022 Jul 16;12(1):12197. PMID: 35842458 -
Oncol Rep
Berberine exerts its antineoplastic effects by reversing the Warburg effect via downregulation of the Akt/mTOR/GLUT1 signaling pathway. [Abstract]2021 Dec;46(6):253. PMID: 34643248 -
J Biol Chem
The adaptor protein GIPC1 stabilizes the scavenger receptor SR-B1 and increases its cholesterol uptake. [Abstract]2021 Jan-Jun:296:100616. PMID: 33811857 -
Biochim Biophys Acta Mol Cell Res
2023 Jan 24;1870(3):119433. PMID: 36706922 -
Toxicol Appl Pharmacol
Inhibition of CDK9 exhibits anticancer activity in hepatocellular carcinoma cells via targeting ribonucleotide reductase. [Abstract]2023 Jul 15:471:116568. PMID: 37245555 -
Chem Asian J
Selective Protein Degradation through Tetrazine Ligation of Genetically Incorporated Unnatural Amino Acids. [Abstract]2024 Sep 2:e202400824. PMID: 39221720 -
J Inorg Biochem
Iridium(III) complexes as type I photosensitizers for hypoxic two-photon photodynamic therapy. [Abstract]2025 Nov:272:113006. PMID: 40682924 -
Environ Toxicol
1-Benzylimidazole attenuates the stemness of breast cancer cells through partially targeting CYP4Z1. [Abstract]2024 Mar;39(3):1505-1520. PMID: 37994574 -
Biochem Biophys Res Commun
Structure-based artificial intelligence-aided design of MYC-targeting degradation drugs for cancer therapy. [Abstract]2025 Apr 21:766:151870. PMID: 40288261 -
STAR Protoc
Protocol for reconstituting enzymatic activities for ultra-large histone methyltransferases NSD1 and SETD2 using a baculovirus expression system. [Abstract]2025 Jul 18;6(3):103963. PMID: 40684435 -
bioRxiv
OSTM1 is a ubiquitin E3 ligase that suppresses B-cell malignancy by activating the cAMP/PKA/CREB pathway. [Abstract]2026 Jan 26:2026.01.23.701155. PMID: 41659680 -
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Purity & Documentation
References
[1]. Aoyagi T, et al. Biological activities of leupeptins. J Antibiot (Tokyo). 1969 Nov;22(11):558-68. [Content Brief]
[2]. 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. [Content Brief]
[3]. Haspel J, et al. Characterization of macroautophagic flux in vivo using a leupeptin-based assay. Autophagy. 2011 Jun;7(6):629-42. [Content Brief]
[4]. Aoyagi T, et al. Biological activities of leupeptins. J Antibiot (Tokyo). 1969 Nov;22(11):558-68.
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)