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).

• Synonyme(s) : Calpeptin, Benzyloxycarbonylleucyl-norleucinal
• Formule empirique (notation de Hill): C₂₀H₃₀N₂O₄
• Numéro CAS: 117591-20-5
• Poids moléculaire : 362.46
• Numéro MDL: MFCD00155623
• Code UNSPSC : 12352202
• Nomenclature NACRES : NA.77

Propriétés

• Niveau de qualité: 100
• Pureté: ≥94% (HPLC)
• Forme: solid
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze
• Couleur: white to off-white
• Solubilité: DMF: 5 mg/mL; DMSO: 5 mg/mL
• Conditions d'expédition: ambient
• Température de stockage: −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
• Clé InChI: PGGUOGKHUUUWAF-ROUUACIJSA-N

Description

Description générale

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.

Actions biochimiques/physiologiques

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

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Standard Handling (A)

Séquence

Z-Leu-Nle-CHO

Notes préparatoires

Dissolve in a minimal amount of DMF or DMSO then add H₂O, buffer or medium just prior to use.

Autres remarques

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.

Informations légales

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable