Pepstatin acetate
Based on 59 publication(s) in Google Scholar
Pepstatin (Pepstatin A) acetate is a specific, orally active aspartic protease inhibitor produced by actinomycetes, with IC50s of 4.5 nM, 6.2 nM, 150 nM, 290 nM, 520 nM and 260 nM for hemoglobin-pepsin, hemoglobin-proctase, casein-pepsin, casein-proctase, casein-acid protease and hemoglobin-acid protease, respectively. Pepstatin acetate also inhibits HIV protease.
For research use only. We do not sell to patients.
- CAS No.: 28575-34-0
- Formula: C36H67N5O11
- Molecular Weight:745.94
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Pepstatin acetate
More- Signal Transduct Target Ther. 2025 Dec 17;10(1):413. [Abstract]
- Nature. 2024 Aug;632(8025):686-694. [Abstract]
- Nature. 2024 Aug;632(8026):930-937. [Abstract]
- Cell. 2025 Nov 26;188(24):6861-6872.e14. [Abstract]
- Cell Res. 2026 Mar 16.
- Cell Res. 2025 May;35(5):385-388. [Abstract]
- ACS Nano. 2024 Jul 2;18(26):16790-16807. [Abstract]
- ACS Nano. 2024 Jan 23;18(3):2162-2183. [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]
- Cell Death Differ. 2026 Jan 28. [Abstract]
- Autophagy. 2025 Jul;21(7):1591-1607. [Abstract]
- Adv Sci (Weinh). 2026 May;13(25):e15367. [Abstract]
- Adv Sci (Weinh). 2025 Aug 7:e09208. [Abstract]
- Adv Sci (Weinh). 2023 Oct;10(28):e2302130. [Abstract]
- Adv Sci (Weinh). 2022 Oct 10;e2203831. [Abstract]
- Theranostics. 2024 Jul 22;14(11):4481-4498. [Abstract]
- Sci Adv. 2026 Jan 30;12(5):eadz8234. [Abstract]
- Carbohydr Polym. 2023 Nov 1:319:121208. [Abstract]
- Sci Adv. 2022 Nov 11;8(45):eabn6579. [Abstract]
- Redox Biol. 2024 Apr:70:103064. [Abstract]
- Environ Sci Technol. 2017 Dec 5;51(23):13938-13948. [Abstract]
- Pharmacol Res. 2022 Jan:175:105985. [Abstract]
- Cancer Lett. 2026 Apr 1:642:218277. [Abstract]
- Cancer Lett. 2022 Jun 1:535:215629. [Abstract]
- Cell Death Dis. 2022 Dec 16;13(12):1048. [Abstract]
- Free Radic Biol Med. 2025 Apr 23:S0891-5849(25)00247-3. [Abstract]
- Br J Pharmacol. 2025 May;182(10):2310-2331. [Abstract]
- Cell Rep. 2025 Jan 15;44(1):115219. [Abstract]
- Cell Rep. 2021 Nov 2;37(5):109931. [Abstract]
- J Anim Sci Biotechnol. 2026 Mar 14;17(1):49. [Abstract]
- Protein Sci. 2024 Dec;33(12):e5225. [Abstract]
- PLoS Pathog. 2025 Oct 17;21(10):e1013581. [Abstract]
- PLoS Pathog. 2024 Feb 14;20(2):e1011981. [Abstract]
- Int J Oncol. 2019 Jul;55(1):331-339. [Abstract]
- Pharmaceuticals (Basel). 2022 Dec 3;15(12):1509. [Abstract]
- Eur J Pharmacol. 2022 Apr 5:920:174823. [Abstract]
- Int J Antimicrob Agents. 2019 Dec;54(6):814-819. [Abstract]
- Mol Pharm. 2024 May 9. [Abstract]
- Immunotargets Ther. 2025 Mar 4:14:151-173. [Abstract]
- Structure. 2025 Dec 4;33(12):2049-2057.e5. [Abstract]
- FASEB J. 2022 Jan;36(1):e22121. [Abstract]
- J Virol. 2023 Nov 30;97(11):e0107523. [Abstract]
- J Virol. 2021 Nov 23;95(24):e0153721. [Abstract]
- PLoS Genet. 2025 Jul 10;21(7):e1011794. [Abstract]
- Mol Med Rep. 2019 Jan;19(1):41-50. [Abstract]
- Toxicol Appl Pharmacol. 2018 Oct 1;356:159-171. [Abstract]
- Arch Biochem Biophys. 2023 Jul 15:743:109646. [Abstract]
- Biochem Biophys Res Commun. 2024 Jun 15:725:150271. [Abstract]
- Biochem Bioph Res Co. 2020 Sep 10;530(1):292-300. [Abstract]
- Biol Pharm Bull. 2022 Apr 1;45(4):438-445. [Abstract]
- STAR Protoc. 2025 Jul 18;6(3):103963. [Abstract]
- bioRxiv. 2025 Dec 26.
- Maastricht University. 2025.
- bioRxiv. 2024 November 14.
- bioRxiv. 2023 Nov 5.
- SSRN. 2023 Apr 10.
Customer Validation & Images
-
WB
-
Cell Imaging/Staining
-
Cell Imaging/Staining
-
Cell Proliferation/Viability Assay
-
WB
Biological Activity
IC50: 4.5 nM (Hemoglobin-pepsin), 6.2 nM (Hemoglobin-proctase), 150 nM (Casein-pepsin), 260 nM (Hemoglobin-acid protease), 290 nM (Casein-proctase), 520 nM (Casein-acid protease)[1]
Pepstatin (Pepstatin A) (7 μM; 48 h) affects the intracellular processing of HIV-specific gag protein[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pepstatin (0.5-50 mg/kg, p.o.) suppresses stomach ulceration of the pylorus in ligated Shay rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Pylorus ligated male Wistar rats[1]
-
Dosage:0.5, 1, 10 and 50 mg/kg
-
Administration:Oral administration, 15 minutes after pyloric ligation
-
Result:Effectively prevented stomach ulceration.
Chemical Information
-
CAS No. 28575-34-0
-
Molecular Weight 745.94
-
Formula C36H67N5O11
-
Synonyms
Pepstatin A acetate
-
Sequence Shortening
{Ac}-VV-{Sta}-A-{Sta}
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (59)
-
Journal Impact Factor
-
Most Recent
-
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 -
Nature
2024 Aug;632(8025):686-694. PMID: 39112701 -
Nature
2024 Aug;632(8026):930-937. PMID: 39085602 -
Cell
2025 Nov 26;188(24):6861-6872.e14. PMID: 41138730 -
-
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 -
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 -
ACS Nano
Ligand Phase Separation-Promoted, "Squeezing-Out" Mode Explaining the Mechanism and Implications of Neutral Nanoparticles That Escaped from Lysosomes. [Abstract]2024 Jan 23;18(3):2162-2183. PMID: 38198577 -
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
Pepstatin acetate purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Nov 19;16(1):10181. [Abstract]
WB analyses of LC3 and p62 levels in cells after indicated treatments for 8 h. The relative levels of LC3 and p62 were showed. 3-MA (3-Methyladenine, 10 mM), CQ (Chloroquine, 20 μM), PA (Pepstatin A,10 μg/mL), LP (Leupeptin, 100 μM), Rapa (Rapamycin, 10 nM).
Pepstatin acetate purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Nov 19;16(1):10181. [Abstract]
Co-immunofluorescence of PRDX1 (red) and LC3 (green) in WT TM3 cells. Cells were treated with or without Chloroquine (20 μM), Pepstatin A (10 μg/mL), or Leupeptin (100 μM) for 8 hours.
-
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 -
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 -
Autophagy
2025 Jul;21(7):1591-1607. PMID: 39952286
Pepstatin acetate purchased from MedChemExpress. Usage Cited in: Autophagy. 2025 Jul;21(7):1591-1607. [Abstract]
Representative fluorescence image of tfLC3 under Pepstatin A + E64d condition in primary liver cells from tfLC3-KI mice.
-
Adv Sci (Weinh)
Cuproptosis and Disulfidptosis Converge to Empower PD-L1 Checkpoint Therapy via Cadict-Induced PD-L1 Translation. [Abstract]2026 May;13(25):e15367. PMID: 41722054 -
Adv Sci (Weinh)
2025 Aug 7:e09208. PMID: 40776529 -
Adv Sci (Weinh)
Palmitoyltransferase ZDHHC3 Aggravates Nonalcoholic Steatohepatitis by Targeting S-Palmitoylated IRHOM2. [Abstract]2023 Oct;10(28):e2302130. PMID: 37544908 -
Adv Sci (Weinh)
The Endoplasmic Reticulum ATP13A1 is Essential for MAVS-Mediated Antiviral Innate Immunity. [Abstract]2022 Oct 10;e2203831. PMID: 36216581
Pepstatin acetate purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2022 Oct 10;e2203831. [Abstract]
Wild-type and ATP13A1−/− HEK293T cells were treated with Bafilomycin A1 (200 nM), E-64d (10 µg/mL) or Pepstatin A (10 µg/mL) for 12 h before immunoblotting analysis.
-
Theranostics
Endosome-microautophagy targeting chimera (eMIATAC) for targeted proteins degradation and enhance CAR-T cell anti-tumor therapy. [Abstract]2024 Jul 22;14(11):4481-4498. PMID: 39113807 -
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
Agrocybe cylindracea fucoglucogalactan induced lysosome-mediated apoptosis of colorectal cancer cell through H3K27ac-regulated cathepsin D. [Abstract]2023 Nov 1:319:121208. PMID: 37567726
Pepstatin acetate purchased from MedChemExpress. Usage Cited in: Carbohydr Polym. 2023 Nov 1:319:121208. [Abstract]
The viability of HCT-116 cells pretreated with 5 μM Pepstatin A was detected by CCK8.
-
Sci Adv
Heightened apoptotic priming of vascular cells across tissues and life span predisposes them to cancer therapy-induced toxicities. [Abstract]2022 Nov 11;8(45):eabn6579. PMID: 36351019 -
Redox Biol
SELENOK-dependent CD36 palmitoylation regulates microglial functions and Aβ phagocytosis. [Abstract]2024 Apr:70:103064. PMID: 38320455 -
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 -
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 -
Cancer Lett
Succinate dehydrogenase B palmitoylation promotes T cell exhaustion through the H3K27ac-PD1 axis in pancreatic cancer. [Abstract]2026 Apr 1:642:218277. PMID: 41577075 -
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
Neuronal haemoglobin induces loss of dopaminergic neurons in mouse Substantia nigra, cognitive deficits and cleavage of endogenous α-synuclein. [Abstract]2022 Dec 16;13(12):1048. PMID: 36526614 -
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 -
Br J Pharmacol
7 I, a structurally modified sinomenine, exerts dual anti-GBM effects by inhibiting glioblastoma proliferation and inducing necroptosis which further mediates lysosomal cell death. [Abstract]2025 May;182(10):2310-2331. PMID: 40038493 -
Cell Rep
Menin orchestrates macrophage reprogramming to maintain the pulmonary immune homeostasis. [Abstract]2025 Jan 15;44(1):115219. PMID: 39817905 -
Cell Rep
2021 Nov 2;37(5):109931. PMID: 34731621 -
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 -
Protein Sci
Distinct substrate specificities of the three catalytic subunits of the Trichomonas vaginalis proteasome. [Abstract]2024 Dec;33(12):e5225. PMID: 39589076 -
PLoS Pathog
HBV p22-interacting protein C1QBP inhibits viral replication through impeding nucleocapsid formation and nuclear import. [Abstract]2025 Oct 17;21(10):e1013581. PMID: 41105696 -
PLoS Pathog
The HN protein of Newcastle disease virus induces cell apoptosis through the induction of lysosomal membrane permeabilization. [Abstract]2024 Feb 14;20(2):e1011981. PMID: 38354122 -
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 -
Pharmaceuticals (Basel)
Toosendanin Induces Hepatocyte Damage by Inhibiting Autophagic Flux via TFEB-Mediated Lysosomal Dysfunction. [Abstract]2022 Dec 3;15(12):1509. PMID: 36558960
Pepstatin acetate purchased from MedChemExpress. Usage Cited in: Pharmaceuticals (Basel). 2022 Dec 3;15(12):1509. [Abstract]
TSN (10 μM), Baf (0.5 μM), and E64D (25 μM) plus pepstatin A (50 μM; E + P ) treatment significantly inhibits the degradation ability of lysosomes (in HepG2 cells and L02 cells; medium for 6 h).
-
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 J Antimicrob Agents
2019 Dec;54(6):814-819. PMID: 31479744 -
Mol Pharm
Saponin and Ribosome-Inactivating Protein Synergistically Trigger Lysosome-Dependent Apoptosis by Inhibiting Lysophagy: Potential to Become a New Antitumor Strategy. [Abstract]2024 May 9. PMID: 38722865 -
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 -
Structure
2025 Dec 4;33(12):2049-2057.e5. PMID: 40914153 -
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
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
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 -
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 -
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 -
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 -
Biochem Biophys Res Commun
Structural insights into the allosteric effects of the antiepileptic drug topiramate on the CaV2.3 channel. [Abstract]2024 Jun 15:725:150271. PMID: 38901222 -
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 -
Biol Pharm Bull
Inhibition of Stearoyl-CoA Desaturase 1 Potentiates Anti-tumor Activity of Amodiaquine in Non-small Cell Lung Cancer. [Abstract]2022 Apr 1;45(4):438-445. PMID: 35110426 -
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 -
-
-
-
-
Purity & Documentation
References
[1]. Umezawa H, et al. Pepstatin, a new pepsin inhibitor produced by Actinomycetes. J Antibiot (Tokyo). 1970 May;23(5):259-62. [Content Brief]
[2]. Seelmeier S, et al. Human immunodeficiency virus has an aspartic-type protease that can be inhibited by pepstatin A. Proc Natl Acad Sci U S A. 1988 Sep;85(18):6612-6. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Powered by Bioz