Pepstatin A

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    Pepstatin A is a well-known inhibitor of aspartic proteinases with IC50 values of 15 μM, 2 μM, <5 nM and <40 nM for human renin, HIV protease, pepsin and cathepsin D, respectively [1, 2].
    Pepstatin A is a pentapeptide. It was originally isolated from the microbe. As a most potent renin inhibitor, pepstatinA inhibited porcine renin and human renin at weak acid pH value with IC50 values of 0.32 and 15 μM, respectively. The disadvantage is that, pepstatin Ais hydrophobic. To couple the charged hydrophilic residues to the C-terminal of pepstatinA can increase its solubility. Besides the renin, pepstatin A was also reported to have inhibitory effects on HIV protease and subsequently suppressed the virus replication. In cultured H9 cells, pepstatinA treatment blocked the proteolytic processing of the virus gag precursor and inhibited the production of infectious HIV. Moreover, pepstatin A was found to inhibit osteoclast differentiation due to its inhibitory efficacy of cathepsin D and E [1, 3 and 4].
    
    1. Eid M, Evin G, Castro B, et al.New renin inhibitors homologous with pepstatin.Biochem. J, 1981, 197: 465-471.
    2. Sarubbi E, Seneci P F, Angelastro M R, et al. Peptide aldehydes as inhibitors of HIV protease. FEBS letters, 1993, 319(3): 253-256.
    3. von der Helm K, Gürtler L, Eberle J, et al. Inhibition of HIV replication in cell culture by the specific aspartic protease inhibitor pepstatin A. FEBS letters, 1989, 247(2): 349-352.
    4. Yoshida H, Okamoto K, Iwamoto T, et al. Pepstatin A, an aspartic proteinase inhibitor, suppresses RANKL-induced osteoclast differentiation. Journal of biochemistry, 2006, 139(3): 583-590.
- Properties
  - Alternative Name
    
    Pepstatin A,NSC272671,Isoval-Val-Val-Sta-Ala-Sta; 3-hydroxy-4-[2-[[3-hydroxy-6-methyl-4-[[3-methyl-2-[[3-methyl-2-(3-methylbutanoylamino)butanoyl]amino]butanoyl]amino]heptanoyl]amino]propanoylamino]-6-methylheptanoic acid
    
    CAS Number
    
    26305-03-3
    
    Molecular Formula
    
    C34H63N5O9
    
    Molecular Weight
    
    685.9
    
    Appearance
    
    A solid
    
    Purity
    
    98.62%
    
    Solubility
    
    ≥34.3 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. HeLia, GuanghuiDanga, et al. "Characterization of a novel Mycobacterium tuberculosis serine protease (Rv3194c) activity and pathogenicity." Tuberculosis. Available online 4 November 2019, 101880.
    2. Ying Long, Xuri Zhang, et al. "Initial events in the breakthrough of the epithelial barrier of the small intestine by Angiostrongylus cantonensis." Arch Biol Sci. 2016;68(2):375-383

We Also Recommend

AEBSF.HCl

$188

Aprotinin

$145

Bestatin

$281

Bestatin

$274

Bestatin

$145

Pepstatin A

Background

We Also Recommend

AEBSF.HCl

Aprotinin

Bestatin

Bestatin

Bestatin