03-34-0051
Calpeptin
A cell-permeable calpain inhibitor (ID₅₀ = 52 nM for calpain-1; ID₅₀ = 34 nM for calpain-2; ID₅₀ = 138 nM for papain).
Synonym(s):
Calpeptin, Benzyloxycarbonylleucyl-norleucinal
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About This Item
Empirical Formula (Hill Notation):
C20H30N2O4
CAS Number:
Molecular Weight:
362.46
MDL number:
UNSPSC Code:
12352202
NACRES:
NA.77
Recommended Products
Quality Level
Assay
≥94% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
color
white to off-white
solubility
DMF: 5 mg/mL
DMSO: 5 mg/mL
shipped in
ambient
storage temp.
−20°C
InChI
1S/C20H30N2O4/c1-4-5-11-17(13-23)21-19(24)18(12-15(2)3)22-20(25)26-14-16-9-7-6-8-10-16/h6-10,13,15,17-18H,4-5,11-12,14H2,1-3H3,(H,21,24)(H,22,25)/t17-,18-/m0/s1
InChI key
PGGUOGKHUUUWAF-ROUUACIJSA-N
General description
Calpeptin inhibits the Ca2+-stimulatedcleavage of p35 to p25 by calpain. It regulates the processing of β-amyloidprecursor protein to β-amyloid (Aβ). Calpeptin alleviates neurite elongation indifferentiating PC12 cells. In platelets, it prevents Ca2+-ionophore-induceddegradation of actin binding protein and P235. It blocks the myosinlight chain phosphorylation in platelets stimulated by collagen, ionomycin, orthrombin. Calpeptin inhibits the growth of estrogen receptor positive breast cancer cells. Calpeptin is a cell permeable calpain blocker. It also blocks theactivation of T-cells in the immune system. It has been observed that calpeptininduces secondary inflammatory responses and apoptosis in muscle cells.
Biochem/physiol Actions
Cell permeable: yes
ID50 = 52 nM for calpain-1; 34 nM for calpain-2; 138 nM for papain
Product does not compete with ATP.
Reversible: no
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Sequence
Z-Leu-Nle-CHO
Preparation Note
Dissolve in a minimal amount of DMF or DMSO then add H₂O, buffer or medium just prior to use.
Other Notes
Lee, M.S., et al. 2000. Nature405, 360.
Yamazaki, T., et al. 1997. Biochemistry27, 8377.
Klafki, H., et al. 1996. J. Biol. Chem.271, 28655.
Shiba, E., et al. 1996. Anticancer Res. 16, 773.
Pinter, M., et al. 1994. Neurosci. Lett. 170, 91.
Saito, K., and Nixon, R.A. 1993. Neurochem. Res. 18, 231.
Tsujinaka, T., et al. 1988. Biochem. Biophys. Res. Commun.153, 1201.
Yamazaki, T., et al. 1997. Biochemistry27, 8377.
Klafki, H., et al. 1996. J. Biol. Chem.271, 28655.
Shiba, E., et al. 1996. Anticancer Res. 16, 773.
Pinter, M., et al. 1994. Neurosci. Lett. 170, 91.
Saito, K., and Nixon, R.A. 1993. Neurochem. Res. 18, 231.
Tsujinaka, T., et al. 1988. Biochem. Biophys. Res. Commun.153, 1201.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Certificates of Analysis (COA)
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Jingjing Zuo et al.
Pathology, research and practice, 214(8), 1199-1209 (2018-08-07)
Exposure to cigarette smoke including secondhand smoking is the most important risk factor in the development of chronic obstructive pulmonary disease where incidence has substantially increased in recent decades. The mechanisms responsible for cigarette smoke-induced pulmonary inflammation remain unclear, and
L Rodríguez-Fernández et al.
Scientific reports, 11(1), 16339-16339 (2021-08-13)
Calpain-2 (CAPN2) is a processing enzyme ubiquitously expressed in mammalian tissues whose pleiotropic functions depend on the role played by its cleaved-products. Nuclear interaction networks, crucial for a number of molecular processes, could be modified by CAPN2 activity. However, CAPN2
Marta Surbek et al.
Scientific reports, 13(1), 21550-21550 (2023-12-07)
Transglutaminase 1 (TGM1) plays an essential role in skin barrier formation by cross-linking proteins in differentiated keratinocytes. Here, we established a protocol for the antibody-dependent detection of TGM1 protein and the parallel detection of TGM activity. TGM1 immunoreactivity initially increased
Archna Sharma et al.
Molecular neurobiology, 60(6), 3311-3328 (2023-03-01)
Abnormal calcium homeostasis, activation of protease calpain, generation of p25 and hyperactivation of cyclin-dependent kinase 5 (Cdk5) have all been implicated in the pathogenesis of neurogenerative diseases including Alzheimer's disease. We have recently shown that extracellular cold-inducible RNA-binding protein (eCIRP)
Jin-Eun Kim et al.
Oncology reports, 49(3) (2023-02-18)
Colon cancer is one of the most frequent malignant neoplasms worldwide. Epidemiological studies suggested that the development of colon cancer can be prevented by plant‑derived ingredients. In the present study, the chemopreventive activity of buddlejasaponin IV (BS‑IV), isolated from the
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