1. Metabolic Enzyme/Protease
    Autophagy
  2. Proteasome
    HIV Protease
    Autophagy
  3. Pepstatin

Pepstatin (Synonyms: Pepstatin A)

Cat. No.: HY-P0018 Purity: >98.0%
Handling Instructions

Pepstatin is a specific 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 Ammonium also inhibits HIV protease.

For research use only. We do not sell to patients.

Pepstatin Chemical Structure

Pepstatin Chemical Structure

CAS No. : 26305-03-3

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10 mg USD 60 In-stock
Estimated Time of Arrival: December 31
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Based on 5 publication(s) in Google Scholar

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Description

Pepstatin is a specific 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 Ammonium also inhibits HIV protease.

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 is a specific acid 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[1]. Pepstatin (Pepstatin A) inhibits the recombinant HIV protease with an IC50 of 250 μM. Pepstatin shows no effect on cellular protein synthesis and probably does not exert severe cell toxicity[2].

In Vivo

Pepstatin 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. Pepstatin (0.5-50 mg/kg, p.o.) suppresses stomach ulceration of the pylorus in ligated Shay rats[1].

Molecular Weight

685.89

Formula

C₃₄H₆₃N₅O₉

CAS No.

26305-03-3

Sequence

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

Sequence Shortening

IsoVeryl-VV-Sta-A-Sta-OH

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -80°C 2 years
  -20°C 1 year
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 25 mg/mL (36.45 mM)

*"≥" means soluble, but saturation unknown.

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
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[2]

Pepstatin A is freshly dissolved in DMSO at 7 mM. It is very slowly diluted (1:100) into the medium of HIV-infected H9 suspension cultures so that no pepstatin A precipitated (final concentration, 70 μM pepstatin A and 1% DMSO), and the cultures are incubated without change of culture medium for 48 hr. As control, uninfected H9 cells are also incubated with pepstatin and in addition HIV infected and uninfected cells are incubated with 1% DMSO but without pepstatin[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Pepstatin
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