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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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).
Submit a review for this product and receive 15 CruzCredits

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.


References

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 :
Solid
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 :
3
PubChem CID :
73364
MDL Number :
MFCD00155623
SMILES :
CCCC[C@@H](C=O)NC(=O)[C@H](CC(C)C)NC(=O)OCC1=CC=CC=C1

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Certificate of Analysis

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Calpeptin  Product 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. J. Nutr. Biochem. 34: 89-98.

PMID: # 26196320  2015. Oncotarget. 6: 27440-60.

PMID: # 25467131  Formisano, L. et al. 2015. J. Pharmacol. Exp. Ther. 352: 236-43.

PMID: # 26103422  Olson, ML. et al. 2015. Brain Sci. 5: 241-57.

PMID: # 25253721  Sako-Kubota, K. et al. 2014. Mol. Biol. Cell. 25: 3851-60.

PMID: # 24482122  Konze, S.A. et al. 2014. Molecular & cellular proteomics : MCP. 13: 990-1007.

PMID: # 23448293  Chau, DM. et al. 2013. Comb. Chem. High Throughput Screen. 16: 415-24.

PMID: # 23934019  2013. J. Assist. Reprod. Genet. 30: 1279-88.

PMID: # 21693630  Formisano, L. et al. 2011. J. Pharmacol. Exp. Ther. 338: 997-997-10031003.

PMID: # 21478251  Sayner, SL. et al. 2011. 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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