Revision 1

#98806Store at -20C

5 mg

Cell Signaling Technology

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For Research Use Only. Not for Use in Diagnostic Procedures.

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).

  1. Umezawa, H. et al. (1970) J Antibiot (Tokyo) 23, 259-62.
  2. Zóia, M.A.P. et al. (2019) Int J Mol Sci 20, 1337. doi: 10.3390/ijms20061337.
  3. Kobayashi, S. et al. (2020) Biochem Biophys Res Commun 523, 239-245.
  4. Yoshida, H. et al. (2006) J Biochem 139, 583-90.
  5. Sarubbi, E. et al. (1993) FEBS Lett 319, 253-6.
  6. 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

Store lyophilized at -20ºC, desiccated. In lyophilized form, the chemical is stable for 24 months. Once in solution, store at -20ºC and use within 2 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

Directions for Use

Pepstatin A is supplied as a lyophilized powder. For a 10 mM stock, reconstitute 5 mg of powder in 0.73 mL of DMSO. Working concentrations and length of treatment can vary depending on the desired effect.

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

    Trademarks and Patents

    Cell Signaling Technology is a trademark of Cell Signaling Technology, Inc.
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    Revision 1
    #98806

    Pepstatin A

    Pepstatin A: Image 1 Expand Image
    胃蛋白酶抑制剂 A 的化学结构。