Pepstatin A
SIGMA/77170 - ≥100,000 U/mg
CAS Number: 26305-03-3
Empirical Formula (Hill Notation): C34H63N5O9
Molecular Weight: 685.89
EC Number: 247-600-0
MDL Number: MFCD00060740
Linear Formula: C34H63N5O9
Product Type: Chemical
| biological source | Streptomyces sp. |
| form | powder |
| InChI | 1S/C34H63N5O9/c1-17(2)12- |
| InChI key | FAXGPCHRFPCXOO-LXTPJMTPSA |
| mp | 233 °C (dec.) (lit.) |
| Quality Level | 100  |
| SMILES string | CC(C)C[C@H](NC(=O)[C@H](C |
| solubility | ethanol: soluble 1 mg/mL |
| specific activity | ≥100,000 U/mg |
| storage temp. | 2-8°C |
| Application: | Pepstatin A is suitable for use: • in the inhibitor cocktail in fluorometric matrix metalloproteinase assay • as a protease inhibitor during homogenization of tissue • as a protease inhibitor during extraction of cells • to determine the molar concentrations of cathepsin D by titration with pepstatin A • in inhibiting cathepsin D It can be used in conjunction with E64-d and Leupeptin A to inhibit the degradation of autophagic cargo inside autophagosomes. For this application, the working concentration is typically between 1-10 μM. |
| Biochem/physiol Actions: | Pepstatin A is an inhibitor of acid proteases (aspartyl peptidases). It forms a 1:1 complex with proteases such as pepsin, renin, cathepsin D, bovine chymosin, and protease B (Aspergillus niger). The inhibitor is highly selective and does not inhibit thiol proteases, neutral proteases, or serine proteases. Solubilized γ-secretase and retroviral protease are also inhibited by Pepstatin A. It has been used to characterize proteases from several sources. |
| Biochem/physiol Actions: | Potent inhibitor of acid proteases, including pepsin, renin and cathepsin D and many microbial aspartic proteases. Effective concentration 1 μM. Stable for about 1 day. |
| Other Notes: | 1 U corresponds to the amount of inhibitor which reduces the activity of pepsin by 1 U (1 U corresponds to the amount of enzyme which increases the absorbance at 280 nm by 0.001 per minute at pH 2.0 and 37°C (Hemoglobin, Cat. No. 51290, as substrate, in an endvolume of 16 ml)); 10′000 absorbance-U as described above are equivalent to ∼1 Bergmeyer-U (when 1 pepsin-U is the amount of enzyme which hydrolyzes 1 μmol acetyl-L-phenylalanyl-3,5 |
| Other Notes: | Strong inhibitor of acid proteases - pepsin, cathepsin D, renin |
| Preparation Note: | Pepstatin can be dissolved at 1 mg/ml in 10% (v/v) acetic acid in methanol (9:1 methanol:acetic acid). The inclusion of acetic acid may be necessary to dissolve this peptide in methanol or DMSO. It has been dissolved at 1 to 2 mg/ml in ethanol, but heat may be required for complete dissolution. Solutions of Pepstatin A can be heated as high as 60 °C without any decomposition of the peptide. Stock solutions at 1 mg/ml are stable at least a week at 4 °C. A 1 mM solution in methanol or DMSO is stable for months at -20 °C. If solutions become darker yellow, the reagent is hydrolyzing. A working concentration of 1 μM is stable for at least one day at room temperature. |
| RIDADR | NONH for all modes of transport |
| WGK Germany | WGK 2 |
| Flash Point(F) | Not applicable |
| Flash Point(C) | Not applicable |
| activity | specific activity: ≥100,000 U/mg |
| mp | 233 °C (dec.) (lit.) |
| Storage Temp. | 2-8°C |
| UNSPSC | 12352202 |