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

ペプスタチン  (Synonyms: Pepstatin; Pepstatin A; ペプスタチン A)

製品番号: HY-P0018 純度: 99.90%
COA 取扱説明書 Technical Support

Pepstatin (Pepstatin A) 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 also inhibits HIV protease.

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カスタムペプチド

CAS 番号 : 26305-03-3

容量 価格(税別) 在庫状況 数量
>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 63 在庫あり
Solution
10 mM * 1 mL in DMSO USD 63 在庫あり
Solid
5 mg $42 在庫あり
10 mg $66 在庫あり
25 mg $132 在庫あり
50 mg $224 在庫あり
100 mg $335 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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カスタマーレビュー

Based on 59 publication(s) in Google Scholar

Other Forms of Pepstatin:

Top Publications Citing Use of Products

顧客検証

WB
Cell Proliferation/Viability Assay
Cell Imaging/Staining
IF

    Pepstatin 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 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 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 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 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 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).
    • 生物活性

    • 純度とドキュメンテーション

    • 参考文献

    • カスタマーレビュー

    製品説明

    Pepstatin (Pepstatin A) 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 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]

    Cellular Effect
    Cell Line Type Value Description References
    CCRF-CEM EC50
    150 μM
    Compound: Pepstatin A
    Antiviral activity against HIV1 Rojo in human CEM cells
    Antiviral activity against HIV1 Rojo in human CEM cells
    [PMID: 11430019]
    CCRF-CEM EC50
    69 μM
    Compound: Pepstatin A
    Antiviral activity against HIV1 RF in human CEM cells
    Antiviral activity against HIV1 RF in human CEM cells
    [PMID: 11430019]
    H9 EC50
    51.8 μM
    Compound: Pepstatin A
    Antiviral activity against HIV1 RF in human H9 cells assessed as inhibition of virus-induced cytopathic effect by formazan-based conventional colorimetric technique
    Antiviral activity against HIV1 RF in human H9 cells assessed as inhibition of virus-induced cytopathic effect by formazan-based conventional colorimetric technique
    [PMID: 11430019]
    MCF7 IC50
    5 nM
    Compound: Pepstatin A
    Inhibition of cathepsin D in human MCF7 cells by fluorescence assay
    Inhibition of cathepsin D in human MCF7 cells by fluorescence assay
    [PMID: 19715320]
    MCF7 IC50
    5 nM
    Compound: Pepstatin A
    Inhibition of cathepsin E in human MCF7 cells by fluorescence assay
    Inhibition of cathepsin E in human MCF7 cells by fluorescence assay
    [PMID: 19715320]
    MCF7 IC50
    5 μM
    Compound: Pepstatin A
    Inhibition of cathepsin D in human MCF7 cells treated for 1 hr measured after washout and trypsin treatment by fluorescence assay
    Inhibition of cathepsin D in human MCF7 cells treated for 1 hr measured after washout and trypsin treatment by fluorescence assay
    [PMID: 19715320]
    MCF7 IC50
    5 μM
    Compound: Pepstatin A
    Inhibition of cathepsin E in human MCF7 cells treated for 1 hr measured after washout and trypsin treatment by fluorescence assay
    Inhibition of cathepsin E in human MCF7 cells treated for 1 hr measured after washout and trypsin treatment by fluorescence assay
    [PMID: 19715320]
    体外実験

    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.

    体内実験

    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.
    分子量

    685.89

    分子式

    C34H63N5O9

    CAS 番号
    Appearance

    Solid

    Color

    White to off-white

    Sequence

    IsoValeryl-Val-Val-Sta-Ala-Sta-OH

    Sequence Shortening

    IsoVeryl-VV-Sta-A-Sta-OH

    Structure Classification
    Initial Source

    actinomycetes

    輸送条件

    Room temperature in continental US; may vary elsewhere.

    保管条件
    Sealed storage, away from moisture
    Powder -80°C 2 years
      -20°C 1 year
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : 31.25 mg/mL (45.56 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.4580 mL 7.2898 mL 14.5796 mL
    5 mM 0.2916 mL 1.4580 mL 2.9159 mL
    10 mM 0.1458 mL 0.7290 mL 1.4580 mL
    View the 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    一般には略語で表示されます:C1V1 = C2V2

    濃度 (開始)

    C1

    ×
    体積 (開始)

    V1

    =
    濃度 (終了)

    C2

    ×
    体積 (終了)

    V2

    体内:

    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.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: 2.08 mg/mL (3.03 mM); Clear solution; Need ultrasonic

      This protocol yields a clear solution of 2.08 mg/mL.

      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.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.08 mg/mL (3.03 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    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.

    • Protocol 1

      Add each solvent one by one:  50% PEG300    50% Saline

      Solubility: 5 mg/mL (7.29 mM); Suspended solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    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).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    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.
    純度とドキュメンテーション

    純度: 99.90%

    参考文献

    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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.4580 mL 7.2898 mL 14.5796 mL 36.4490 mL
    5 mM 0.2916 mL 1.4580 mL 2.9159 mL 7.2898 mL
    10 mM 0.1458 mL 0.7290 mL 1.4580 mL 3.6449 mL
    15 mM 0.0972 mL 0.4860 mL 0.9720 mL 2.4299 mL
    20 mM 0.0729 mL 0.3645 mL 0.7290 mL 1.8224 mL
    25 mM 0.0583 mL 0.2916 mL 0.5832 mL 1.4580 mL
    30 mM 0.0486 mL 0.2430 mL 0.4860 mL 1.2150 mL
    40 mM 0.0364 mL 0.1822 mL 0.3645 mL 0.9112 mL
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    • Molarity Calculator

    • Dilution Calculator

    The molarity calculator equation

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    質量   濃度   体積   分子量 *
    = × ×

    The dilution calculator equation

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    一般には略語で表示されます:C1V1 = C2V2

    濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
    × = ×
    C1   V1   C2   V2
    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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    製品名:
    Pepstatin
    製品番号:
    HY-P0018
    数量:
    MCE 日本正規代理店: