Pepstatin A #98806
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Product Description
| Molecular Weight | 685.9 g/mol |
| Purity | >98% |
| Molecular Formula | C34H63N5O9 |
| CAS | 26305-03-3 |
| Solubility | Soluble in DMSO at 5 mg/mL or ethanol at 1 mg/mL. |
Background
Pepstatin A is a low molecular weight inhibitor of aspartyl proteases, including pepsin, renin, cathepsin D and cathepsin E (1). Cathepsin D is a ubiquitously expressed lysosomal aspartyl protease involved in the normal degradation of proteins; dysregulation of cathepsin D plays a role in neuronal degradation and malignant transformation. Cathespin D is highly expressed in triple-negative breast cancer (TNBC) cells. Pepstatin A treatment induced apoptosis and autophagy while reducing the proliferation, invasion, and migration of TNBC cells (2). Increased expression and leakage of lysosomal cathepsin D is associated with cardiomyocyte death related to hyperglycemia. Treatment with Pepstatin A markedly diminished high glucose-induced cardiomyocyte death (3). Pepstatin A treatment of osteoclast cells suppressed receptor activator of NF-κB ligand (RANKL)-induced differentiation to mononuclear osteoclast cells by blocking NFATc1 expression and inhibiting ERK signaling (4). Pepstatin A also inhibits human immunodeficiency virus (HIV) protease (5). Pepstatin A treatment of HIV-infected H9 cells decreased the level of HIV core antigen in the culture medium (6).
- Umezawa, H. et al. (1970) J Antibiot (Tokyo) 23, 259-62.
- Zóia, M.A.P. et al. (2019) Int J Mol Sci 20, 1337. doi: 10.3390/ijms20061337.
- Kobayashi, S. et al. (2020) Biochem Biophys Res Commun 523, 239-245.
- Yoshida, H. et al. (2006) J Biochem 139, 583-90.
- Sarubbi, E. et al. (1993) FEBS Lett 319, 253-6.
- von der Helm, K. et al. (1989) FEBS Lett 247, 349-52.
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