Pepstatin (Synonyms: Pepstatin A)

Name: Pepstatin
Brand: MedChemExpress
SKU: HY-P0018
Rating: 5.0 (59 reviews)

Cat. No.: HY-P0018 Pureza: 99.90%: Ficha de datos
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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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Síntesis de péptidos personalizados

No. CAS : 26305-03-3

Tamaño	Stock	Cantidad

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	En stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	En stock	Estimated Time of Arrival: December 31
Solid
5 mg	En stock	Estimated Time of Arrival: December 31
10 mg	En stock	Estimated Time of Arrival: December 31
25 mg	En stock	Estimated Time of Arrival: December 31
50 mg	En stock	Estimated Time of Arrival: December 31
100 mg	En stock	Estimated Time of Arrival: December 31
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Revisión del cliente

Based on 59 publication(s) in Google Scholar

Other Forms of Pepstatin:

Pepstatin Trifluoroacetate In-stock
Pepstatin Ammonium In-stock
Pepstatin acetate Obtener un presupuesto
Pepstatin (Standard) Obtener un presupuesto

59 Publications Citing Use of MCE Pepstatin

Cell Proliferation/Viability Assay

Cell Imaging/Staining

: 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).

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Descripciòn

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 3 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 3 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 3 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]
CCRF-CEM	EC₅₀	69 3 Compound: Pepstatin A	Antiviral activity against HIV1 RF in human CEM cells Antiviral activity against HIV1 RF in human CEM cells	[PMID: 11430019]
CCRF-CEM	EC₅₀	150 3 Compound: Pepstatin A	Antiviral activity against HIV1 Rojo in human CEM cells Antiviral activity against HIV1 Rojo in human CEM cells	[PMID: 11430019]
MCF7	IC₅₀	5 1 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 1 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 1 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]
H9	EC₅₀	51.8 3 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 3 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 3 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 3 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]
H9	EC₅₀	51.8 3 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 1 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 1 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 3 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 3 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]

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.

Peso molecular

685.89

Fòrmula

C₃₄H₆₃N₅O₉

No. CAS

26305-03-3

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

Others

Initial Source

Microorganisms

actinomycetes

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Sealed storage, away from moisture

Powder	-80°C	2 years
	-20°C	1 year

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

Solvente y solubilidad

In Vitro:

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.

Calculadora de molaridad
Calculadora de dilución

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (3.03 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

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)

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.

Pureza y Documentación

Purity: 99.90%

Select Batch:

Ficha de datos (278 KB) SDS (393 KB)

COA (255 KB) HNMR (320 KB) RP-HPLC (244 KB) MS (69 KB) Elemental Analysis Report (113 KB)

Instrucciones de manejo (2659 KB)

Referencias

[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]

Complete Stock Solution Preparation Table

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

Pepstatin Related Classifications

Inflammation/Immunology Infection

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.

Keywords:

Pepstatin26305-03-3Pepstatin AHIV ProteaseAutophagyaspartic proteaseorally activehemoglobin-pepsinhemoglobin-proctasecasein-pepsincasein-proctasecasein-acid proteasehemoglobin-acid proteaseHIV proteaseInhibitorinhibitorinhibit

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Pepstatin (Synonyms: Pepstatin A)

Revisión del cliente

Other Forms of Pepstatin:

Pepstatin Related Antibodies

59 Publications Citing Use of MCE Pepstatin

Recomendaciones destacadas

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Actividad biológica

Pureza y Documentación

Referencias

Revisión del cliente

Pepstatin Related Antibodies

Calculadora de molaridad

Calculadora de dilución

Complete Stock Solution Preparation Table

Pepstatin Related Classifications

Keywords:

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