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Pepstatin

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].

Product Specifications

CAS Number

[26305-03-3]

Product Name Alternative

Pepstatin A

UNSPSC

12352209

Hazard Statement

H315, H319, H335

Target

Autophagy; HIV Protease

Type

Peptides

Related Pathways

Anti-infection; Autophagy; Metabolic Enzyme/Protease

Applications

COVID-19-anti-virus

Field of Research

Infection; Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/Pepstatin.html

Purity

99.90

Solubility

DMSO : 31.25 mg/mL (ultrasonic)

Smiles

CC(C[C@H](NC([C@@H](NC([C@@H](NC(CC(C)C)=O)C(C)C)=O)C(C)C)=O)[C@@H](O)CC(N[C@@H](C)C(N[C@@H](CC(C)C)[C@@H](O)CC(O)=O)=O)=O)C

Molecular Formula

C34H63N5O9

Molecular Weight

685.89

Precautions

H315, H319, H335

References & Citations

[1]Umezawa H, et al. Pepstatin, a new pepsin inhibitor produced by Actinomycetes. J Antibiot (Tokyo) . 1970 May;23 (5) :259-62.|[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.

Shipping Conditions

Blue Ice

Storage Conditions

-80°C, 2 years; -20°C, 1 year (Powder, sealed storage, away from moisture)

Scientific Category

Peptides

Clinical Information

No Development Reported

Citation 01

ACS Nano. 2024 Jul 2;18 (26) :16790-16807.|Adv Sci (Weinh) . 2022 Oct 10; e2203831.|Adv Sci (Weinh) . 2023 Oct;10 (28) :e2302130.|Adv Sci (Weinh) . 2025 Aug 7:e09208.|Arch Biochem Biophys. 2023 Jul 15:743:109646.|Autophagy. 2025 Jul;21 (7) :1591-1607.|Biochem Bioph Res Co. 2020 Sep 10;530 (1) :292-300.|Biochem Biophys Res Commun. 2024 Jun 15:725:150271.|bioRxiv. 2023 Nov 5.|bioRxiv. 2024 November 14.|Br J Pharmacol. 2025 May;182 (10) :2310-2331.|Cancer Lett. 2022 Jun 1:535:215629.|Carbohydr Polym. 2023 Nov 1:319:121208.|Cell Death Dis. 2022 Dec 16;13 (12) :1048.|Cell Rep. 2021 Nov 2;37 (5) :109931.|Cell Rep. 2025 Jan 15;44 (1) :115219.|Cell. 2025 Oct 24:S0092-8674 (25) 01131-6.|Environ Sci Technol. 2017 Dec 5;51 (23) :13938-13948.|Eur J Pharmacol. 2022 Apr 5:920:174823.|FASEB J. 2022 Jan;36 (1) :e22121.|Free Radic Biol Med. 2025 Aug 1:235:95-108.|Immunotargets Ther. 2025 Mar 4:14:151-173.|Int J Oncol. 2019 Jul;55 (1) :331-339.|J Virol. 2021 Nov 23;95 (24) :e0153721.|J Virol. 2023 Nov 30;97 (11) :e0107523.|Maastricht University. 2025.|Mol Med Rep. 2019 Jan;19 (1) :41-50.|Mol Pharm. 2024 May 9.|Nat Commun. 2025 Apr 2;16 (1) :3153.|Nat Commun. 2025 Jul 16;16 (1) :6551.|Nat Commun. 2025 Mar 11;16 (1) :2412.|Nat Commun. 2025 Nov 19;16 (1) :10181.|Nature. 2024 Aug;632 (8025) :686-694.|Nature. 2024 Aug;632 (8026) :930-937.|Pharmaceuticals (Basel) . 2022 Dec 3;15 (12) :1509.|Pharmacol Res. 2022 Jan:175:105985.|PLoS Genet. 2025 Jul 10;21 (7) :e1011794.|PLoS Pathog. 2024 Feb 14;20 (2) :e1011981.|PLoS Pathog. 2025 Oct 17;21 (10) :e1013581.|Protein Sci. 2024 Dec;33 (12) :e5225.|Redox Biol. 2024 Apr:70:103064.|Sci Adv. 2022 Nov 11;8 (45) :eabn6579.|SSRN. 2023 Apr 10.|STAR Protoc. 2025 Jul 18;6 (3) :103963.|Structure. 2025 Sep 5.|Theranostics. 2024 Jul 22;14 (11) :4481-4498.|Toxicol Appl Pharmacol. 2018 Oct 1;356:159-171. |ACS Nano. 2024 Jan 23;18 (3) :2162-2183.|Int J Antimicrob Agents. 2019 Dec;54 (6) :814-819.|Biol Pharm Bull. 2022 Apr 1;45 (4) :438-445.

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