Biochem/physiol Actions

Reversible: no

Product does not compete with ATP.

Cell permeable: yes

ID50 = 52 nM for calpain-1; 34 nM for calpain-2; 138 nM for papain

General description

A cell-permeable calpain inhibitor. Inactivates calpain I (ID₅₀ = 52 nM), calpain II (ID₅₀ = 34 nM), and papain (ID₅₀ = 138 nM). Promotes neurite elongation in differentiating PC12 cells. Prevents Ca²⁺-ionophore induced degradation of actin binding protein and P₂₃₅ in platelets. Inhibits myosin light chain phosphorylation in platelets stimulated by collagen, ionomycin, or thrombin. Inhibits the growth of estrogen receptor positive breast cancer cells.

A cell-permeable calpain inhibitor (ID₅₀ = 52 nM for calpain-1; ID₅₀ = 34 nM for calpain-2; ID₅₀ = 138 nM for papain). Inhibits the Ca²⁺-stimulated cleavage of p35 to p25 by calpain. Modulates the processing of β-amyloid precursor protein to β-amyloid (Aβ). Promotes neurite elongation in differentiating PC12 cells. Prevents Ca²⁺-ionophore-induced degradation of actin binding protein and P₂₃₅ in platelets. Inhibits myosin light chain phosphorylation in platelets stimulated by collagen, ionomycin, or thrombin. Inhibits the growth of estrogen receptor positive breast cancer cells.

Legal Information

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

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.

Packaging

Packaged under inert gas

Preparation Note

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

Sequence

Z-Leu-Nle-CHO

Warning

Toxicity: Standard Handling (A)