1. Anti-infection Metabolic Enzyme/Protease Autophagy
  2. HIV Protease Autophagy
  3. Pepstatin acetate

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.

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CAS No. : 28575-34-0

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Top Publications Citing Use of Products

59 Publications Citing Use of MCE Pepstatin acetate

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Cell Proliferation/Viability Assay
Cell Imaging/Staining
IF

    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.

    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.

    Pepstatin acetate purchased from MedChemExpress. Usage Cited in: Carbohydr Polym. 2023 Nov 1:319:121208.

    The viability of HCT-116 cells pretreated with 5 μM Pepstatin A was detected by CCK8.

    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.

    Pepstatin acetate purchased from MedChemExpress. Usage Cited in: Pharmaceuticals (Basel). 2022 Dec 3;15(12):1509.

    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).
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    Description

    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[1][2].

    IC50 & Target

    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]

    In Vitro

    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.

    In Vivo

    Pepstatin (Pepstatin A) has a very low toxicity, with LD50s of 1090 mg/kg, 875 mg/kg, 820 mg/kg and 450 mg/kg for mice, rats, rabbits, and dogs by i.p. route, and > 2000 mg/kg for all species by oral route[1].
    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.
    Molecular Weight

    745.94

    Formula

    C36H67N5O11

    CAS No.
    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.

    Purity & Documentation
    References
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    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Product Name:
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    Cat. No.:
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