Date published: 2025-11-1

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Calpeptin (CAS 117591-20-5)

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Alternate Names:
Z-Leu-norleucinal; N-Benzyloxycarbonyl-L-leucyl-norleucinal
Application:
Calpeptin is a calpain-2, cathepsin L, and calpain-1 inhibitor
CAS Number:
117591-20-5
Purity:
≥98%
Molecular Weight:
362.5
Molecular Formula:
C20H30N2O4
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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Calpeptin is a cell permeable calpain inhibitor. Research shows that it is an effective inhibitor of calpain 2 and can fully block cleavage of PLC-beta 3 enzymes. Additionally, Calpeptin has demonstrated the ability to inhibit the activities of cathepsin L and calpain-1. In muscle cell studies, it blocked the expression of aspartyl protease cathepsin D, amyloid precursor protein, and calparin. Pulmonary fibrosis research in mice have reported that Calpeptin can decrease expression of TGF-beta1, IL-6, collage type Ialpha1, and angiopoietin-1 mRNA. Calpeptin is an inhibitor of Calpain 1, cathepsin K, cathepsin L and PTP, and an activator of Rock.


Calpeptin (CAS 117591-20-5) References

  1. Protease inhibitors: current status and future prospects.  |  Leung, D., et al. 2000. J Med Chem. 43: 305-41. PMID: 10669559
  2. Exploration of the P1 SAR of aldehyde cathepsin K inhibitors.  |  Catalano, JG., et al. 2004. Bioorg Med Chem Lett. 14: 275-8. PMID: 14684342
  3. Design of small molecule ketoamide-based inhibitors of cathepsin K.  |  Catalano, JG., et al. 2004. Bioorg Med Chem Lett. 14: 719-22. PMID: 14741275
  4. Calpain inhibition attenuates intracellular changes in muscle cells in response to extracellular inflammatory stimulation.  |  Nozaki, K., et al. 2010. Exp Neurol. 225: 430-5. PMID: 20673830
  5. The calpain inhibitor calpeptin prevents bleomycin-induced pulmonary fibrosis in mice.  |  Tabata, C., et al. 2010. Clin Exp Immunol. 162: 560-7. PMID: 20846163
  6. The repressor element 1-silencing transcription factor is a novel molecular target for the neurotoxic effect of the polychlorinated biphenyl mixture aroclor 1254 in neuroblastoma SH-SY5Y cells.  |  Formisano, L., et al. 2011. J Pharmacol Exp Ther. 338: 997-1003. PMID: 21693630
  7. Calpeptin Reduces Neurobehavioral Deficits and Neuronal Apoptosis Following Subarachnoid Hemorrhage in Rats.  |  Zhou, YD. and Cai, L. 2019. J Stroke Cerebrovasc Dis. 28: 125-132. PMID: 30337208
  8. Anti-SARS-CoV-2 Activity of Extracellular Vesicle Inhibitors: Screening, Validation, and Combination with Remdesivir.  |  Kongsomros, S., et al. 2021. Biomedicines. 9: PMID: 34572416
  9. Calpain Inhibitor Calpeptin Alleviates Ischemia/Reperfusion-Induced Acute Kidney Injury via Suppressing AIM2 Inflammasome and Upregulating Klotho Protein.  |  Wu, Y., et al. 2022. Front Med (Lausanne). 9: 811980. PMID: 35155498
  10. Calpain Inhibitor Calpeptin Improves Alzheimer's Disease-Like Cognitive Impairments and Pathologies in a Diabetes Mellitus Rat Model.  |  Li, M., et al. 2022. Neurotox Res. 40: 1248-1260. PMID: 36018506
  11. Morin post-treatment surpassed calpeptin in ameliorating 3-NP-induced cortical neurotoxicity via modulation of glutamate/calpain axis, Kidins220, and BDNF/TrkB/AKT/CREB trajectory.  |  Mohamed, OE., et al. 2023. Int Immunopharmacol. 116: 109771. PMID: 36736222
  12. Endogenous cleavage of phospholipase C-beta 3 by agonist-induced activation of calpain in human platelets.  |  Banno, Y., et al. 1995. J Biol Chem. 270: 4318-24. PMID: 7876193
  13. Role of intracellular proteases in differentiation of L6 myoblast cells.  |  Ebisui, C., et al. 1994. Biochem Mol Biol Int. 32: 515-21. PMID: 8032318
  14. Comparison of the effect of calpain inhibitors on two extralysosomal proteinases: the multicatalytic proteinase complex and m-calpain.  |  Figueiredo-Pereira, ME., et al. 1994. J Neurochem. 62: 1989-94. PMID: 8158145
  15. Subsite requirements for peptide aldehyde inhibitors of human calpain I  |  Mohamed Iqbal, Patricia A. Messina, etc. 1997. Bioorganic & Medicinal Chemistry Letters. 7: 539 -544.

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

Calpeptin, 10 mg

sc-202516
10 mg
$119.00

Calpeptin, 50 mg

sc-202516A
50 mg
$447.00

I am trying to assess concentration of calpeptin that should be used in our in vitro studies: many papers mention a concentration of 1U/ml, however, there is no information re enzyme unit coming with your product. Could you please comment/advise? Many tha

Asked by: nickname123
Thank you for your question. The enzyme activity of sc-202516 has not been tested.
Answered by: Technical Support
Date published: 2017-12-07

Is this product stable at 4˚C? 

Asked by: hawkeye11
This chemical, Calpeptin (CAS 117591-20-5), is stable for about a month at 4˚C.
Answered by: Chemical Support 1
Date published: 2017-03-15
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Rated 5 out of 5 by from FormisanoFormisano, L. et al. (PubMed 21693630) found that Calpeptin, a cell permeable calpain inhibitor, prevented cell death from exposure to Aroclor 1254. -SCBT Publication Review
Date published: 2015-03-08
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Calpeptin is rated 5.0 out of 5 by 1.
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