Aloxistatin
Based on 90 publication(s) in Google Scholar
Aloxistatin (E64d) is a cell-permeable and irreversible broad-spectrum cysteine protease inhibitor. Aloxistatin (E64d) exhibits entry-blocking effect for MERS-CoV.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.94%
- CAS. Nr.: 88321-09-9
- Formel: C17H30N2O5
- Molecular Weight:342.43
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Publications Citing Use of MedChemExpress (MCE) Aloxistatin
More- Signal Transduct Target Ther. 2025 Dec 17;10(1):413. [Abstract]
- Signal Transduct Target Ther. 2021 Mar 27;6(1):134. [Abstract]
- Cancer Cell. 2021 Mar 8;39(3):423-437.e7. [Abstract]
- Nat Cell Biol. 2026 Apr;28(4):812-827. [Abstract]
- Nat Microbiol. 2025 Nov;10(11):2860-2874. [Abstract]
- Nat Microbiol. 2024 Sep;9(9):2383-2394. [Abstract]
- Autophagy. 2025 Jul;21(7):1591-1607. [Abstract]
- Autophagy. 2025 May;21(5):934-956. [Abstract]
- Autophagy. 2023 Jun;19(6):1745-1763. [Abstract]
- Nat Commun. 2025 Dec 11;16(1):11002. [Abstract]
- Nat Commun. 2024 Oct 4;15(1):8622. [Abstract]
- Nat Commun. 2024 Oct 9;15(1):8728. [Abstract]
- Nat Commun. 2024 Jan 2;15(1):162. [Abstract]
- Nat Commun. 2021 Sep 17;12(1):5498. [Abstract]
- Nat Commun. 2020 Mar 27;11(1):1620. [Abstract]
- ACS Nano. 2024 Jul 2;18(26):16790-16807. [Abstract]
- Cell Discov. 2021 Dec 14;7(1):119. [Abstract]
- Redox Biol. 2024 Apr:70:103064. [Abstract]
- Nat Plants. 2025 Sep 12. [Abstract]
- Nucleic Acids Res. 2021 Jan 8;49(D1):D1113-D1121. [Abstract]
- Adv Sci (Weinh). 2022 Oct 10;e2203831. [Abstract]
- Cell Rep Med. 2022 Sep 20;3(9):100743. [Abstract]
- Sci Adv. 2023 Jan 20;9(3):eadd3867. [Abstract]
- Plant Commun. 2024 Sep 13:101135. [Abstract]
- Cell Death Differ. 2026 Jan 28. [Abstract]
- Plant Biotechnol J. 2025 Dec 17. [Abstract]
- Plant Biotechnol J. 2025 Jun 8. [Abstract]
- Pharmacol Res. 2022 Jan:175:105985. [Abstract]
- Environ Sci Technol. 2017 Dec 5;51(23):13938-13948. [Abstract]
- Cell Commun Signal. 2023 Apr 21;21(1):83. [Abstract]
- EBioMedicine. 2023 Sep:95:104753. [Abstract]
- Proc Natl Acad Sci U S A. 2022 Nov;119(44):e2214227119. [Abstract]
- New Phytol. 2022 Dec;236(6):2202-2215. [Abstract]
- Free Radic Biol Med. 2025 Apr 23:S0891-5849(25)00247-3. [Abstract]
- J Anim Sci Biotechnol. 2026 Mar 14;17(1):49. [Abstract]
- Cell Rep. 2026 Apr 21;45(5):117295. [Abstract]
- Emerg Microbes Infect. 2023 Dec;12(1):2207688. [Abstract]
- Emerg Microbes Infect. 2022 Dec;11(1):2275-2287. [Abstract]
- Emerg Microbes Infect. 2022 Dec;11(1):483-497. [Abstract]
- Front Immunol. 2021 Apr 23:12:642855. [Abstract]
- Plant Cell Environ. 2024 Jun 27. [Abstract]
- Ecotoxicol Environ Saf. 2023 Jun 1:257:114947. [Abstract]
- Biochem Pharmacol. 2024 Nov:229:116114. [Abstract]
- Cell Biosci. 2024 Aug 2;14(1):101. [Abstract]
- Stress Biol. 2026 May 6;6(1):35. [Abstract]
- Stress Biol. 2026 Jan 4;6(1):1. [Abstract]
- Pharmaceuticals (Basel). 2022 Dec 3;15(12):1509. [Abstract]
- Eur J Pharmacol. 2022 Apr 5:920:174823. [Abstract]
- Int Immunopharmacol. 2024 Mar 10:129:111594. [Abstract]
- Chem Biol Interact. 2021 Feb 25;336:109319. [Abstract]
- Mol Med Rep. 2019 Jan;19(1):41-50. [Abstract]
- PLoS Pathog. 2025 Oct 14;21(10):e1013593. [Abstract]
- Sci Rep. 2022 Jul 16;12(1):12197. [Abstract]
- PLoS Pathog. 2021 Mar 4;17(3):e1009370. [Abstract]
- Antiviral Res. 2023 Jun:214:105606. [Abstract]
- FASEB J. 2022 Jan;36(1):e22121. [Abstract]
- J Virol. 2025 Aug 11:e0105525. [Abstract]
- J Virol. 2025 Apr 25:e0000225. [Abstract]
- Immunotargets Ther. 2025 Mar 4:14:151-173. [Abstract]
- J Virol. 2024 Nov 19;98(11):e0075424. [Abstract]
- J Virol. 2023 Nov 30;97(11):e0107523. [Abstract]
- J Virol. 2023 Aug 31;97(8):e0085123. [Abstract]
- J Virol. 2021 Nov 23;95(24):e0153721. [Abstract]
- PLoS Genet. 2025 Jul 10;21(7):e1011794. [Abstract]
- Biochim Biophys Acta Mol Cell Biol Lipids. 2026 Jan;1871(1):159705. [Abstract]
- Vet Res. 2024 Sep 27;55(1):124. [Abstract]
- Viruses. 2022 Jun 23;14(7):1369. [Abstract]
- Dis Model Mech. 2026 Feb 1;19(2):dmm052582. [Abstract]
- Toxicol Appl Pharmacol. 2018 Oct 1;356:159-171. [Abstract]
- Arch Biochem Biophys. 2023 Jul 15:743:109646. [Abstract]
- Vaccines. 2020 Jan 13;8(1):22. [Abstract]
- Biosaf Health. 2022 Feb;4(1):38-44. [Abstract]
- PLoS One. 2019 Dec 30;14(12):e0227278. [Abstract]
- Biochem Bioph Res Co. 2020 Sep 10;530(1):292-300. [Abstract]
- Biochem Biophys Res Commun. 2018 Sep 3;503(1):297-303. [Abstract]
- bioRxiv. 2026 Jun 14:2026.06.10.731244. [Abstract]
- bioRxiv. 2026 May 7.
- Patent. US20250123269A1.
- Heidelberg University. 2025.
- Res Sq. 2025 Feb 25.
- bioRxiv. 2024 September 09.
- Authorea. 2024 May 5.
- bioRxiv. 2024 Mar 9:2024.03.07.583938. [Abstract]
- bioRxiv. 2023 Nov 5.
- Res Sq. 2023 Sep 11:rs.3.rs-3220157. [Abstract]
- bioRxiv. 2023 Aug 2:2023.07.31.551381. [Abstract]
- Elife. 2021 Jan 4:10:e64508. [Abstract]
- bioRxiv. 2021 Jan 22.
- bioRxiv. 2020 Jun.
- bioRxiv. 2020 Jun.
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Bio/Physico-chemical Assay
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WB
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IF
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IF
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WB
Alle Cathepsin Isoform-spezifische Produkte anzeigen
More
Biologische Aktivität
Cysteine protease[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| U-937 | IC50 |
1.1 μM
Compound: E-64d
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Blockade of cathepsin G processing in human U937 cells by densitometry
Blockade of cathepsin G processing in human U937 cells by densitometry
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[PMID: 17535802] |
Inhibition of protease-resistant prion protein (PrP-res) accumulation in ScNB cells by cysteine protease inhibitor Aloxistatin (E64d) with IC50 of 0.5±0.11 μM. For the cell surface PrP-sen detection, PrP-sen is immunoprecipitated from media treated with phosphatidylinositol-specific phospholipase C (PIPLC) to release pulse-35S-labeled PrP-sen from the cell surface. Aloxistatin is maintained at 15 μM, respectively, in the labeling media of all but the control cells [1]. Aloxistatin (E64d) (which specifically blocks cysteine proteases, but not serine proteases such as granzymes) is able to completely block turnover of the CatL substrate Z-Phe-Arg-aminomethylcoumarin, when pre-incubated with NK-92 or YT 5 cells[2]. Aloxistatin (E64d) is a broad-spectrum cell-permeable inhibitor of cysteine proteases[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 88321-09-9
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Appearance Solid
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Molecular Weight 342.43
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Formel C17H30N2O5
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Color White to off-white
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SMILES
O=C([C@H]1O[C@@H]1C(N[C@H](C(NCCC(C)C)=O)CC(C)C)=O)OCC
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Synonyms
E64d; E64c ethyl ester
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (90)
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Journal Impact Factor
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Most Recent
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Signal Transduct Target Ther
Disruption of heme homeostasis by nuclear receptor Nur77 induces pyroptosis through granzyme B-dependent GSDMC cleavage. [Abstract]2025 Dec 17;10(1):413. PMID: 41407678 -
Signal Transduct Target Ther
Cathepsin L plays a key role in SARS-CoV-2 infection in humans and humanized mice and is a promising target for new drug development. [Abstract]2021 Mar 27;6(1):134. PMID: 33774649
Aloxistatin purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2021 Mar 27;6(1):134. [Abstract]
Analysis of CTSL-mediated S-protein cleavage. Purified SARS-CoV-1 or SARS-CoV-2 S protein was incubated in the presence or absence (assay buffer, pH = 5.5) of CTSL (2 or 10 μg/ml in assay buffer, pH = 5.5) at 37 °C for 1 h. The reaction system of 2 μg/ml CTSL was further supplemented with CTSL inhibitors (20 μM E64d (Aloxistatin) or 20 μM SID 26681509), as indicated. Proteins were subjected to SDS-PAGE and detected by silver staining.
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Cancer Cell
Cathepsin C promotes breast cancer lung metastasis by modulating neutrophil infiltration and neutrophil extracellular trap formation. [Abstract]2021 Mar 8;39(3):423-437.e7. PMID: 33450198 -
Nat Cell Biol
TOLLIP targets GSDME-NT-carrying endocytic vesicles for autophagy to regulate pyroptosis and chemotherapy efficacy. [Abstract]2026 Apr;28(4):812-827. PMID: 41803502 -
Nat Microbiol
2025 Nov;10(11):2860-2874. PMID: 41168429 -
Nat Microbiol
Evolution of SARS-CoV-2 in the murine central nervous system drives viral diversification. [Abstract]2024 Sep;9(9):2383-2394. PMID: 39179693
Aloxistatin purchased from MedChemExpress. Usage Cited in: Nat Microbiol. 2024 Sep;9(9):2383-2394. [Abstract]
Vero-E6 cells expressing hACE2 and TMPRSS2 were challenged with WT or ΔFCS pseudotyped virus in the presence of aloxistatin at increasing concentrations (0-100 μM). After 48h of infection, cells were lysed, and luciferase expression was quantified. Relative luciferase expression was normalized to untreated cells. The data are presented as the mean percentages of inhibition across six wells. P-values comparing curve fit of WT and ΔFCS viruses are reported.
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Autophagy
2025 Jul;21(7):1591-1607. PMID: 39952286 -
Autophagy
2025 May;21(5):934-956. PMID: 39663580 -
Autophagy
The Valsa mali effector Vm1G-1794 protects the aggregated MdEF-Tu from autophagic degradation to promote infection in apple. [Abstract]2023 Jun;19(6):1745-1763. PMID: 36449354 -
Nat Commun
Pathogenicity, virological features, and immune evasion of SARS-CoV-2 JN.1-derived variants including JN.1.7, KP.2, KP.3, and KP.3.1.1. [Abstract]2025 Dec 11;16(1):11002. PMID: 41381428 -
Nat Commun
Plekhg5 controls the unconventional secretion of Sod1 by presynaptic secretory autophagy. [Abstract]2024 Oct 4;15(1):8622. PMID: 39366938
Aloxistatin purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Oct 4;15(1):8622. [Abstract]
Elevated Sod1 levels in the medium upon lysosomal dysfunction. Western blots of lysates and media from NSC34 cells treated with Pepstatin A and Aloxistatin (E64d) (10 µg/mL) for 8 h.
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Nat Commun
Lineage-specific pathogenicity, immune evasion, and virological features of SARS-CoV-2 BA.2.86/JN.1 and EG.5.1/HK.3. [Abstract]2024 Oct 9;15(1):8728. PMID: 39379369 -
Nat Commun
Tubeimosides are pan-coronavirus and filovirus inhibitors that can block their fusion protein binding to Niemann-Pick C1. [Abstract]2024 Jan 2;15(1):162. PMID: 38167417 -
Nat Commun
A CRISPR/Cas9 genetically engineered organoid biobank reveals essential host factors for coronaviruses. [Abstract]2021 Sep 17;12(1):5498. PMID: 34535662 -
Nat Commun
Characterization of spike glycoprotein of SARS-CoV-2 on virus entry and its immune cross-reactivity with SARS-CoV. [Abstract]2020 Mar 27;11(1):1620. PMID: 32221306 -
ACS Nano
Realistic Nanoplastics Induced Pulmonary Damage via the Crosstalk of Ferritinophagy and Mitochondrial Dysfunction. [Abstract]2024 Jul 2;18(26):16790-16807. PMID: 38869479
Aloxistatin purchased from MedChemExpress. Usage Cited in: ACS Nano. 2024 Jul 2;18(26):16790-16807. [Abstract]
TC-1 cells were pretreated with Aloxistatin (E64d) (29 μM)/Pepstatin (14 μM) for 1 h, followed by NP treatment for 24 h. Immunofluorescence results showed that E64d/Pepstatin pretreatment increased the colocalization ratio of FTH1 and NCOA4 in the NP treatment group (n = 3).
Aloxistatin purchased from MedChemExpress. Usage Cited in: ACS Nano. 2024 Jul 2;18(26):16790-16807. [Abstract]
TC-1 cells were pretreated with Aloxistatin (E64d) (29 μM)/Pepstatin A (14 μM) for 1 h, followed by NPs treatment for 24 h. Representative immunofluorescence images and co-localization statistics between FTH1 and LAMP2 in normal and NPs-treated TC-1 cells. Immunofluorescence results showed that E64d/Pepstatin A pretreatment increased the co-localization ratio of FTH1 and LAMP2 in NPs treatment group.
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Cell Discov
SARS-CoV-2 uses metabotropic glutamate receptor subtype 2 as an internalization factor to infect cells. [Abstract]2021 Dec 14;7(1):119. PMID: 34903715 -
Redox Biol
SELENOK-dependent CD36 palmitoylation regulates microglial functions and Aβ phagocytosis. [Abstract]2024 Apr:70:103064. PMID: 38320455 -
Nat Plants
An apoplastic fungal effector disrupts N-glycosylation of ZmLecRK1, inducing its degradation to suppress disease resistance in maize. [Abstract]2025 Sep 12. PMID: 40940425 -
Nucleic Acids Res
COVID19 Drug Repository: text-mining the literature in search of putative COVID19 therapeutics. [Abstract]2021 Jan 8;49(D1):D1113-D1121. PMID: 33166390 -
Adv Sci (Weinh)
The Endoplasmic Reticulum ATP13A1 is Essential for MAVS-Mediated Antiviral Innate Immunity. [Abstract]2022 Oct 10;e2203831. PMID: 36216581 -
Cell Rep Med
2022 Sep 20;3(9):100743. PMID: 36084644 -
Sci Adv
2023 Jan 20;9(3):eadd3867. PMID: 36662861 -
Plant Commun
Phosphorylation of PIP2;7 by CPK28 or Phytophthora kinase effectors dampens pattern-triggered immunity in Arabidopsis. [Abstract]2024 Sep 13:101135. PMID: 39277790 -
Cell Death Differ
TUFT1 stabilizes TGF-β receptor II protein and facilitates activation of hepatic stellate cells into metastasis-promoting myofibroblasts. [Abstract]2026 Jan 28. PMID: 41593321 -
Plant Biotechnol J
A Bacterial Effector Hijacks NBR1 to Modulate Both Autophagy and Ubiquitination-Mediated Degradation That Promotes Bacterial Infection. [Abstract]2025 Dec 17. PMID: 41405133 -
Plant Biotechnol J
RD21 enhances resistance to the strawberry vein banding virus by promoting autophagy-mediated degradation of the viral silencing suppressor P6 protein. [Abstract]2025 Jun 8. PMID: 40483578 -
Pharmacol Res
Lycorine improves peripheral nerve function by promoting Schwann cell autophagy via AMPK pathway activation and MMP9 downregulation in diabetic peripheral neuropathy. [Abstract]2022 Jan:175:105985. PMID: 34863821 -
Environ Sci Technol
Determining the Cytotoxicity of Rare Earth Element Nanoparticles in Macrophages and the Involvement of Membrane Damage. [Abstract]2017 Dec 5;51(23):13938-13948. PMID: 29121463 -
Cell Commun Signal
Gasdermin E regulates the stability and activation of EGFR in human non-small cell lung cancer cells. [Abstract]2023 Apr 21;21(1):83. PMID: 37085908 -
EBioMedicine
The viral fitness and intrinsic pathogenicity of dominant SARS-CoV-2 Omicron sublineages BA.1, BA.2, and BA.5. [Abstract]2023 Sep:95:104753. PMID: 37579626 -
Proc Natl Acad Sci U S A
2022 Nov;119(44):e2214227119. PMID: 36279464 -
New Phytol
An F-box protein attenuates fungal xylanase-triggered immunity by destabilizing LRR-RLP NbEIX2 in a SOBIR1-dependent manner. [Abstract]2022 Dec;236(6):2202-2215. PMID: 36151918 -
Free Radic Biol Med
PGAM5 aggravated doxorubicin-induced cardiotoxicity by disturbing mitochondrial dynamics and exacerbating cardiomyocytes apoptosis. [Abstract]2025 Apr 23:S0891-5849(25)00247-3. PMID: 40280314 -
J Anim Sci Biotechnol
AMBRA1 activation alleviates zearalenone-induced swine testicular cell ferroptosis by facilitating mitophagy. [Abstract]2026 Mar 14;17(1):49. PMID: 41826991 -
Cell Rep
Increased yolk lipid mobilization promotes zebrafish post-segmentation growth via an Hnf4-lipoprotein axis. [Abstract]2026 Apr 21;45(5):117295. PMID: 42018437 -
Emerg Microbes Infect
Porcine deltacoronavirus resists antibody neutralization through cell-to-cell transmission. [Abstract]2023 Dec;12(1):2207688. PMID: 37125733 -
Emerg Microbes Infect
Spike mutations contributing to the altered entry preference of SARS-CoV-2 omicron BA.1 and BA.2. [Abstract]2022 Dec;11(1):2275-2287. PMID: 36039901 -
Emerg Microbes Infect
Obatoclax inhibits SARS-CoV-2 entry by altered endosomal acidification and impaired cathepsin and furin activity in vitro. [Abstract]2022 Dec;11(1):483-497. PMID: 34989664 -
Front Immunol
The NLRP3-Inflammasome-Caspase-1 Pathway Is Upregulated in Idiopathic Pulmonary Fibrosis and Acute Exacerbations and Is Inducible by Apoptotic A549 Cells. [Abstract]2021 Apr 23:12:642855. PMID: 33968032 -
Plant Cell Environ
2024 Jun 27. PMID: 38935876 -
Ecotoxicol Environ Saf
Multi-locus deletion mutation induced by silver nanoparticles: Role of lysosomal-autophagy dysfunction. [Abstract]2023 Jun 1:257:114947. PMID: 37105094 -
Biochem Pharmacol
Pharmacological inhibition of cathepsin S and of NSPs-AAP-1 (a novel, alternative protease driving the activation of neutrophil serine proteases). [Abstract]2024 Nov:229:116114. PMID: 39455238 -
Cell Biosci
2024 Aug 2;14(1):101. PMID: 39095802 -
Stress Biol
Reversible S-palmitoylation of C4 protein encoded by TYLCCxV orchestrates geminiviral pathogenesis. [Abstract]2026 May 6;6(1):35. PMID: 42086987 -
Stress Biol
Areca palm velarivirus 1 encoded CP suppresses antiviral RNA silencing by mediating the autophagic degradation of SGS3 and disrupting the SGS3-RDR6 interaction. [Abstract]2026 Jan 4;6(1):1. PMID: 41485154 -
Pharmaceuticals (Basel)
Toosendanin Induces Hepatocyte Damage by Inhibiting Autophagic Flux via TFEB-Mediated Lysosomal Dysfunction. [Abstract]2022 Dec 3;15(12):1509. PMID: 36558960 -
Eur J Pharmacol
Schisandrin B suppresses gastric cancer cell growth and enhances the efficacy of chemotherapy drug 5-FU in vitro and in vivo. [Abstract]2022 Apr 5:920:174823. PMID: 35157912 -
Int Immunopharmacol
The protease inhibitor E64d might attenuate the development of experimental anti-glomerular basement membrane disease through regulating the activation of Th1 cells. [Abstract]2024 Mar 10:129:111594. PMID: 38295547 -
Chem Biol Interact
Swainsonine promotes apoptosis by impairing lysosomal function and inhibiting autophagic degradation in rat primary renal tubular epithelial cells. [Abstract]2021 Feb 25;336:109319. PMID: 33186601 -
Mol Med Rep
Hyperoside decreases the apoptosis and autophagy rates of osteoblast MC3T3‑E1 cells by regulating TNF‑like weak inducer of apoptosis and the p38mitogen activated protein kinase pathway. [Abstract]2019 Jan;19(1):41-50. PMID: 30387825 -
PLoS Pathog
UBXN7 facilitates SARS-CoV-2 replication via inhibiting the K48-linked ubiquitination of viral N protein. [Abstract]2025 Oct 14;21(10):e1013593. PMID: 41086194 -
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 -
PLoS Pathog
The unfolded protein response plays dual roles in rice stripe virus infection through fine-tuning the movement protein accumulation. [Abstract]2021 Mar 4;17(3):e1009370. PMID: 33662041 -
Antiviral Res
Omicsynin B4 potently blocks coronavirus infection by inhibiting host proteases cathepsin L and TMPRSS2. [Abstract]2023 Jun:214:105606. PMID: 37076089 -
FASEB J
PKM2 compensates for proteasome dysfunction by mediating the formation of the CHIP-HSP70-BAG3 complex and the aggregation of ubiquitinated proteins. [Abstract]2022 Jan;36(1):e22121. PMID: 34951719 -
J Virol
Cathepsin L and transmembrane serine protease 11E mediate trypsin-independent entry of porcine deltacoronavirus into Huh7 cells. [Abstract]2025 Aug 11:e0105525. PMID: 40787987 -
J Virol
Syntaxin-6 restricts SARS-CoV-2 infection by facilitating virus trafficking to autophagosomes. [Abstract]2025 Apr 25:e0000225. PMID: 40277356 -
Immunotargets Ther
The Effects of M2 Macrophages-Derived Exosomes on Urethral Fibrosis and Stricture in Scar Formation. [Abstract]2025 Mar 4:14:151-173. PMID: 40061513 -
J Virol
SARS-CoV-2 NSP6 reduces autophagosome size and affects viral replication via sigma-1 receptor. [Abstract]2024 Nov 19;98(11):e0075424. PMID: 39445785 -
J Virol
Coxsackievirus A6 2C protein antagonizes IFN-β production through MDA5 and RIG-I depletion. [Abstract]2023 Nov 30;97(11):e0107523. PMID: 37847581 -
J Virol
SARS-CoV-2 Omicron entry is type II transmembrane serine protease-mediated in human airway and intestinal organoid models. [Abstract]2023 Aug 31;97(8):e0085123. PMID: 37555660 -
J Virol
Inhibition of Autophagy Suppresses SARS-CoV-2 Replication and Ameliorates Pneumonia in hACE2 Transgenic Mice and Xenografted Human Lung Tissues. [Abstract]2021 Nov 23;95(24):e0153721. PMID: 34550769 -
PLoS Genet
2025 Jul 10;21(7):e1011794. PMID: 40638681 -
Biochim Biophys Acta Mol Cell Biol Lipids
Sphinganine-induced lysosomal membrane permeabilization: Interplay with subcellular oxidative levels. [Abstract]2026 Jan;1871(1):159705. PMID: 41213325 -
Vet Res
Development and characterization of reverse genetics systems of feline infectious peritonitis virus for antiviral research. [Abstract]2024 Sep 27;55(1):124. PMID: 39334482 -
Viruses
A Newly Engineered A549 Cell Line Expressing ACE2 and TMPRSS2 Is Highly Permissive to SARS-CoV-2, Including the Delta and Omicron Variants. [Abstract]2022 Jun 23;14(7):1369. PMID: 35891350 -
Dis Model Mech
Enhanced lysosomal exocytosis and altered growth factor signaling are associated with cartilage pathology in a model of mucopolysaccharidosis type IVA. [Abstract]2026 Feb 1;19(2):dmm052582. PMID: 41582713 -
Toxicol Appl Pharmacol
Alantolactone induces apoptosis and improves chemosensitivity of pancreatic cancer cells by impairment of autophagy-lysosome pathway via targeting TFEB. [Abstract]2018 Oct 1;356:159-171. PMID: 30086361
Aloxistatin purchased from MedChemExpress. Usage Cited in: Toxicol Appl Pharmacol. 2018 Oct 1;356:159-171. [Abstract]
Western blot analysis of PARP and cleaved PARP levels MIA PaCa-2 and PANC-1 cells pre-treated with inhibitors of lysosomal hydrolases (Aloxistatin, 5 μM) for 1 h, followed by a 24-h treatment with Alan (20 μM).
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Arch Biochem Biophys
Handelin protects human skin keratinocytes against ultraviolet B-induced photodamage via autophagy activation by regulating the AMPK-mTOR signaling pathway. [Abstract]2023 Jul 15:743:109646. PMID: 37225010 -
Vaccines
Autophagy Promotes Duck Tembusu Virus Replication by Suppressing p62/SQSTM1-Mediated Innate Immune Responses In Vitro. [Abstract]2020 Jan 13;8(1):22. PMID: 31941042 -
Biosaf Health
Establishment of a pseudovirus neutralization assay based on SARS-CoV-2 S protein incorporated into lentiviral particles. [Abstract]2022 Feb;4(1):38-44. PMID: 35005601 -
PLoS One
2019 Dec 30;14(12):e0227278. PMID: 31887216 -
Biochem Bioph Res Co
Selective binding of mitophagy receptor protein Bcl-rambo to LC3/GABARAP family proteins. [Abstract]2020 Sep 10;530(1):292-300. PMID: 32828302 -
Biochem Biophys Res Commun
Effects of intracellular iron overload on cell death and identification of potent cell death inhibitors. [Abstract]2018 Sep 3;503(1):297-303. PMID: 29890135 -
bioRxiv
2026 Jun 14:2026.06.10.731244. PMID: 42327310 -
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bioRxiv
A TLR7 Agonist Conjugated to a Nanofibrous Peptide Hydrogel as a Potent Vaccine Adjuvant. [Abstract]2024 Mar 9:2024.03.07.583938. PMID: 38496534 -
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Res Sq
2023 Sep 11:rs.3.rs-3220157. PMID: 37790412 -
bioRxiv
Growth media affects susceptibility of air-lifted human nasal epithelial cell cultures to SARS-CoV2, but not Influenza A, virus infection. [Abstract]2023 Aug 2:2023.07.31.551381. PMID: 37577692 -
Elife
SARS-CoV-2 entry into human airway organoids is serine protease-mediated and facilitated by the multibasic cleavage site. [Abstract]2021 Jan 4:10:e64508. PMID: 33393462 -
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Lösungsmittel & Löslichkeit
DMSO : 116.67 mg/mL (340.71 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Ethanol : ≥ 33.33 mg/mL (97.33 mM)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% EtOH 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.30 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% EtOH 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.30 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Add each solvent one by one: 10% EtOH 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (7.30 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.08 mg/mL (6.07 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protokoll
Cell proliferation and apoptosis are assessed by staining for a proliferation marker, Ki67, or an apoptotic marker, cleaved caspase 3, following the protocol described above for the polarity markers. MCF10 variants are grown in 3D rBM overlay cultures for 4 days and are treated with 0.1 % DMSO, 5 μM CA074Me or 5 μM Aloxistatin. The percentage of structures that are positive for Ki67 or cleaved caspase 3 is determined by counting a total of 100 structures on two separate coverslips with a Zeiss Axiophot epifluorescent microscope. Structures are considered Ki67 positive if they contained at least one cell staining for Ki67. Structures are considered to be caspase 3 positive if they contained at least one cell that is positive for cleaved caspase 3 and the positive cell(s) is not localized in the center of a developing lumen[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice and Pigs[4]
Guinea Pigs (male, Hartley strain, average weight 400 g corresponding to animals about 6 weeks old) are used. Male transgenic mice expressing human AβPP containing the wt β-secretase site and the London mutant β-secretase site sequences are used. Delivering a drug by gavage offers the advantage of accurate dosing but is traumatic and thus only suitable for relatively short dosing periods (up to about a week). Delivery by gavage is used for the guinea pig studies. Aloxistatin is suspended in Me2SO at the indicated concentrations (0.1, 1.0, 5, and 10 mg/kg) and administered by gavage daily using a feeding tube. Vehicle control animals are treated by gavage of Me2SO alone.
Rats[5]
Male inbred DS rats are used. Weaned rats are fed laboratory chow containing 0.3% NaCl until 7 weeks of age. DS rats fed an 8% NaCl diet after 7 weeks manifest compensated concentric left ventricular (LV) hypertrophy secondary to hypertension at 12 weeks and a distinct stage of fatal LV failure with lung congestion at 19 weeks. DS rats are therefore fed an 8% NaCl diet from 7 weeks of age and are randomized to an HF group, an Aloxistatin group (10 mg per kg of body mass per day, administered intraperitoneally every other day), or an RNH-6270 group (3 mg/kg per day in chow) from 12 to 19 weeks of age (n=10 for each group). The doses of RNH-6270 (an ARB) and Aloxistatin are determined in preliminary experiments and previous studies. DS rats maintained on the 0.3% NaCl diet served as age-matched controls (control group, n=10). At 19 weeks of age, all of the rats are euthanized by an intraperitoneal overdose of NSC 10816 (50 mg/kg), and the hearts are removed for biological and histological analyses. Arterial blood is collected from the abdominal aorta for the measurement of renin activity. Systolic blood pressure and heart rate are measured in conscious rats from 7 weeks of age, every week, using a noninvasive tail-cuff method. In separate experiments, 12-week-old DS rats, fed a low-salt diet from 7 weeks of age, are given vehicle, RNH-6270, or Aloxistatin in the same manner as in the above experiments (n=5 for each group), and the LV tissues for measuring targeting mRNAs and protein levels are immediately placed in liquid nitrogen and stored at -80°C.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (280 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Doh-Ura K, et al. Lysosomotropic agents and cysteine protease inhibitors inhibit scrapie-associated prion protein accumulation. J Virol. 2000 May;74(10):4894-7. [Content Brief]
[2]. Konjar S, et al. Human and mouse perforin are processed in part through cleavage by the lysosomal cysteine proteinase cathepsin L. Immunology. 2010 Oct;131(2):257-67. [Content Brief]
[3]. Mullins SR, et al. Three-dimensional cultures modeling premalignant progression of human breast epithelial cells: role of cysteine cathepsins. Biol Chem. 2012 Dec;393(12):1405-16. [Content Brief]
[4]. Hook G, et al. The cysteine protease inhibitor, E64d, reduces brain amyloid-β and improves memory deficits in Alzheimer's disease animal models by inhibiting cathepsin B, but not BACE1, β-secretase activity. J Alzheimers Dis. 2011;26(2):387-408. [Content Brief]
[5]. Cheng XW, et al. Superoxide-dependent cathepsin activation is associated with hypertensive myocardial remodeling and represents a target for angiotensin II type 1 receptor blocker treatment. Am J Pathol. 2008 Aug;173(2):358-69. [Content Brief]
[6]. Ji Yeun Kim, et al. Safe, High-Throughput Screening of Natural Compounds of MERS-CoV Entry Inhibitors Using a Pseudovirus Expressing MERS-CoV Spike Protein. Int J Antimicrob Agents. 2018 Nov;52(5):730-732. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| Ethanol / DMSO | 1 mM | 2.9203 mL | 14.6015 mL | 29.2030 mL | 73.0076 mL |
| 5 mM | 0.5841 mL | 2.9203 mL | 5.8406 mL | 14.6015 mL | |
| 10 mM | 0.2920 mL | 1.4602 mL | 2.9203 mL | 7.3008 mL | |
| 15 mM | 0.1947 mL | 0.9734 mL | 1.9469 mL | 4.8672 mL | |
| 20 mM | 0.1460 mL | 0.7301 mL | 1.4602 mL | 3.6504 mL | |
| 25 mM | 0.1168 mL | 0.5841 mL | 1.1681 mL | 2.9203 mL | |
| 30 mM | 0.0973 mL | 0.4867 mL | 0.9734 mL | 2.4336 mL | |
| 40 mM | 0.0730 mL | 0.3650 mL | 0.7301 mL | 1.8252 mL | |
| 50 mM | 0.0584 mL | 0.2920 mL | 0.5841 mL | 1.4602 mL | |
| 60 mM | 0.0487 mL | 0.2434 mL | 0.4867 mL | 1.2168 mL | |
| 80 mM | 0.0365 mL | 0.1825 mL | 0.3650 mL | 0.9126 mL | |
| DMSO | 100 mM | 0.0292 mL | 0.1460 mL | 0.2920 mL | 0.7301 mL |