Calpeptin A calpain-2, cathepsin L, and calpain-1 inhibitor

Calpeptin (CAS 117591-20-5)

Calpeptin | CAS 117591-20-5 is rated 5.0 out of 5 by 1.
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| See product citations (11)
Synonym: Z-Leu-norleucinal; N-Benzyloxycarbonyl-L-leucyl-norleucinal
Application: A calpain-2, cathepsin L, and calpain-1 inhibitor
CAS Number: 117591-20-5
Purity: ≥98%
Molecular Weight: 362.5
Molecular Formula: C20H30N2O4
* Refer to Certificate of Analysis for lot specific data (including water content).
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Ordering Information

Calpeptin sc-202516 10 mg $107.00
Calpeptin sc-202516A 50 mg $428.00

Calpeptin is a cell permeable calpain inhibitor. Research shows that Calpeptin is an effective inhibitor of calpain 2 and can fully block cleavage of PLC-β 3 enzymes. Additionally, Calpeptin has demonstrated the ability to inhibit the activities of cathepsin L and calpain-1. In muscle cell studies Calpeptin 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-β1, IL-6, collage type Iα1, and angiopoietin-1 mRNA. Calpeptin is an inhibitor of Calpain 1, cathepsin K, cathepsin L and PTP. Calpeptin is an activator of Rock.


1. Ebisui, C., et al. 1994. Biochem. Mol. Biol. Int. 32: 515-521. PMID: 8032318
2. Figueiredo-Pereira, M.E., et al. 1994. J. Neurochem. 62: 1989-1994. PMID: 8158145
3. Banno, Y. et al. 1995. J. Biol. Chem. 270: 4318-4324. PMID: 7876193
4. Bioorg. Med. Chem. Lett. (1997) 7:539-544
5. Leung, D. et al. 2000. J. Med. Chem. 43(3): 305-341. PMID: 10669559
6. Catalano, J.G. et al. 2004. Bioorg. Med. Chem. Lett. 14(1): 275-278. PMID: 14684342
7. Catalano, J.G. et al. 2004. Bioorg. Med. Chem. Lett. 14(3): 719-722. PMID: 14741275
8. Tabata, C., et al. 2010. Clin Exp Immunol. PMID: 20846163
9. Nozaki, K., et al. 2010. Exp. Neurol. 225: 430-435. PMID: 20673830
10. Formisano, L. et al. 2011. J. Pharmacol. Exp. Ther. 338(3): 997-1003. PMID: 21693630

Usage :
Stock solutions are stable for up to 2 months when stored at - 20°C.
Physical State :
Solubility :
Soluble in DMSO (5 mg/ml), DMF (5 mg/ml), and ethanol (25 mg/ml).
Storage :
Store at -20° C
Melting Point :
86-97° C
Boiling Point :
550.66° C at 760 mmHg (Predicted)
Density :
1.08 g/cm3 (Predicted)
Refractive Index :
n20D 1.51 (Predicted)
IC50 :
Cathepsin K: IC50 = 0.11 nM (human); calpain 10: IC50 = 4 nM (rabbit); calpain 1: IC50 = 5 nM (human)
Ki Data :
Calpain 1: Ki= 7 nM (human)
pK Values :
pKa: 11.14 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
PubChem CID :
MDL Number :

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Certificate of Analysis

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CalpeptinProduct Citations

See how others have used Calpeptin. Click on the entry to view the PubMed entry .

Citations 1 to 10 of 11 total

PMID: # 27239756
Dos Santos, MP. et al. 2016. Higher insulin sensitivity in EDL muscle of rats fed a low-protein, high-carbohydrate diet inhibits the caspase-3 and ubiquitin-proteasome proteolytic systems but does not increase protein synthesis. J. Nutr. Biochem.. 34: 89-98.

PMID: # 26196320
2015. Galeterone and VNPT55 induce proteasomal degradation of AR/AR-V7, induce significant apoptosis via cytochrome c release and suppress growth of castration resistant prostate cancer xenografts in vivo. Oncotarget. 6: 27440-60.

PMID: # 25467131
Formisano, L. et al. 2015. MS-275 inhibits aroclor 1254-induced SH-SY5Y neuronal cell toxicity by preventing the formation of the HDAC3/REST complex on the synapsin-1 promoter. J. Pharmacol. Exp. Ther.. 352: 236-43.

PMID: # 26103422
Olson, ML. et al. 2015. Hippocampal Cortactin Levels are Reduced Following Spatial Working Memory Formation, an Effect Blocked by Chronic Calpain Inhibition. Brain Sci. 5: 241-57.

PMID: # 25253721
Sako-Kubota, K. et al. 2014. Minus end-directed motor KIFC3 suppresses E-cadherin degradation by recruiting USP47 to adherens junctions. Mol. Biol. Cell. 25: 3851-60.

PMID: # 24482122
Konze, S.A. et al. 2014. Cleavage of E-cadherin and β-catenin by calpain affects Wnt signaling and spheroid formation in suspension cultures of human pluripotent stem cells. Molecular & cellular proteomics : MCP.

PMID: # 23448293
Chau, DM. et al. 2013. A novel high throughput 1536-well Notch1 γ -secretase AlphaLISA assay. Comb. Chem. High Throughput Screen.. 16: 415-24.

PMID: # 23934019
2013. Attempted application of bioengineered/biosynthetic supporting matrices with phosphatidylinositol-trisphosphate-enhancing substances to organ culture of human primordial follicles. J. Assist. Reprod. Genet.. 30: 1279-88.

PMID: # 21693630
Formisano, L. et al. 2011. 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. J. Pharmacol. Exp. Ther.. 338: 997-1003.

PMID: # 21478251
Sayner, SL. et al. 2011. Filamin A is a phosphorylation target of membrane but not cytosolic adenylyl cyclase activity. Am. J. Physiol. Lung Cell Mol. Physiol.. 301: L117-24.

Citations 1 to 10 of 11 total

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 Formisano Formisano, 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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