P4265 Sigma

Pepstatin A

microbial, ≥75% (HPLC)




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.


1, 5 mg in glass bottle

25 mg in poly bottle

100, 250 mg in glass bottle

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.

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.

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Safety & Documentation

Safety Information

WGK Germany 
Protocols & Articles
Peer-Reviewed Papers


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Inhibition of aspartic proteases by pepstatin and 3-methylstatine derivatives of pepstatin. Evidence for collected-substrate enzyme inhibition. Rich, D.H., et al. Biochemistry 24, 3165, (1985)


Cellular expression and antimicrobial function of a phylogenetically conserved novel histone 1x-like protein on mouse cells: a potential new class of pattern recognition receptor. Evans, D.L., et al. J. Neurochem. 86, 133-41, (2009)

Cardiac Oxytocin Receptor Blockade Stimulates Adverse Cardiac Remodeling In Ovariectomized Spontaneously Hypertensive Rats. Jankowski, M., et al. Am. J. Physiol. Heart Circ. Physiol. 299, H265-74, (2010)


Preparation of extracts from plants. Gegenheimer, P. Meth. Enzymol. 182, 174-193, (1990)


Maintaining protein stability. Deutscher, M.P Meth. Enzymol. 182, 83-89, (1990)


A gradient of ROR2 protein stability and membrane localization confers brachydactyly type B or Robinow syndrome phenotypes. Schwarzer, W., et al. Hum. Mutat. 18, 4013-21, (2009)


Mechanism Of Interferon-gamma Mediated Down-regulation Of Interleukin-10 Gene Expression. Schaefer, A., et al. Mol. Immunol. 46, 1351-9, (2009)


Role Of Nonspecific Cytotoxic Cells In Bacterial Resistance: Expression Of A Novel Pattern Recognition Receptor With Antimicrobial Activity. Connor, M.A., et al. Mol. Hum. Reprod. 46, 953-61, (2009)


RaPID: An Aptamer-based MRNA Affinity Purification Technique For The Identification Of RNA And Protein Factors Present In Ribonucleoprotein Complexes. Slobodin, B., and Gerst, J.E. Methods Mol. Biol. 714, 387-406, (2011)


Preimplantation embryo development in the mouse requires the latency of TRP53 expression, which is induced by a ligand-activated PI3 kinase/AKT/MDM2-mediated signaling pathway. X.L. Jin et al Biol. Reprod. 80, 286-94, (2008)


A role for the NAD-dependent deacetylase Sirt1 in the regulation of autophagy Lombard, D.B., et al. Proc. Natl. Acad. Sci. U. S. A. 105, 3374-3379, (2008)


Angiotensin II-dependent hypertension increases Na transport-related oxygen consumption by the thick ascending limb. Silva GB Hypertension 52(6), 1091-8, (2008)


Prolyl 3-hydroxylase 1 and CRTAP are mutually stabilizing in the endoplasmic reticulum collagen prolyl 3-hydroxylation complex. Chang W Hum. Mol. Genet. 19(2), 223-34, (2010)


Sequestration of free cholesterol in cell membranes by prions correlates with cytoplasmic phospholipase A2 activation. Bate, C BMC Biol. 6, 8, (2008)


Ginkgolides protect against amyloid-beta1-42-mediated synapse damage in vitro. Bate C Molecular Neurodegeneration 3, 1, (2008)


Glycogen synthase kinase-3 and Omi/HtrA2 induce annexin A2 cleavage followed by cell cycle inhibition and apoptosis. Chi-Yun Wang et al Mol. Biol. Cell 20, 4153-61, (2009)


Effect of oophorectomy and exogenous estrogen replacement on liver injury in experimental obstructive jaundice. Ucan, HB World J. Gastroenterol. 14(18), 2818-24, (2008)


Activation of MEK 1/2 and p42/44 MAPK by angiotensin II in hepatocyte nucleus and their potentiation by ethanol. Annayya R. Aroor et al Alcohol 43, 315-22, (2009)


ROS-mediated autophagy induced by dysregulation of lipid metabolism plays a protective role in colorectal cancer cells treated with gambogic acid. Zhang H, Lei Y, Yuan P, et al. PLoS ONE 9(5), e96418, (2014)


Itraconazole suppresses the growth of glioblastoma through induction of autophagy: involvement of abnormal cholesterol trafficking. Liu R, Li J, Zhang T, et al. Autophagy 10(7), 1241-55, (2014)


Calpain 5 is highly expressed in the central nervous system (CNS), carries dual nuclear localization signals, and is associated with nuclear promyelocytic leukemia protein bodies. Singh R, Brewer MK, Mashburn CB, et al. J. Biol. Chem. 289(28), 19383-94, (2014)


Merck 14,7147

FT-IR 2 (1), 1336:A / RegBook 1 (1), 921:E / Sax 6, 2143 / Structure Index 1, 143:D:2

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