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).
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- Kobayashi, S. et al. (2020) Biochem Biophys Res Commun 523, 239-245.
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- von der Helm, K. et al. (1989) FEBS Lett 247, 349-52.
Molecular Formula
C34H63N5O9
Molecular Weight
685.9 g/mol
Purity
>98%
CAS
26305-03-3
Solubility
Soluble in DMSO at 5 mg/mL or ethanol at 1 mg/mL.
Storage
Directions for Use
Background References
Cross-Reactivity Key
H: human M: mouse R: rat Hm: hamster Mk: monkey Vir: virus Mi: mink C: chicken Dm: D. melanogaster X: Xenopus Z: zebrafish B: bovine Dg: dog Pg: pig Sc: S. cerevisiae Ce: C. elegans Hr: horse GP: Guinea Pig Rab: rabbit All: all species expected
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