Biochem/physiol Actions

Primary Targetcalpain 1, calpain 2

Reversible: yes

Product does not compete with ATP.

Target K_i: 140 nM and 41 nM, against calpain-1 and -2, respectively

Cell permeable: yes

General description

A cell-permeable dipeptidyl a-ketoamide that acts as a potent, highly selective, reversible, active site inhibitor of calpain-1 (K_i = 140 nM) and calpain-2 (K_i = 41 nM). Weakly inhibits cathepsin B (K_i = 6.9 µM). Shown to inhibit calpain-m-mediated degradation of neurofilament protein (NFP) (IC₅₀ = 600 nM). Also shown to exhibit neuroprotective effects in the central nervous system following focal ischemia. Reported to protect against reovirus-induced myocarditis in mice.

A cell-permeable dipeptidyl α-ketoamide that acts as a potent, highly selective, reversible, and active site inhibitor of calpain-1 and -2 (K_i = 140 nM and 41 nM, respectively). Weakly inhibits cathepsin B (K_i = 6.9 µM). Reported to have a neuroprotective role in the central nervous system following focal ischemia. Also protects against virus-induced apoptotic myocardial injury in mice.

Legal Information

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

Other Notes

Blomgren, K., et al. 2001. J. Biol. Chem.276, 10191.DeBiasi, R.L., et al. 2001. J. Virol.75, 351.Saatman, K.E., et al. 2000. J. Cereb. Blood Flow Metab.20, 66.Stelmasiak, Z., et al. 2000. Med. Sci. Monit.6, 426.Blomgren, K., et al. 1999. J. Biol. Chem.274, 14046.James, T., et al. 1998. J. Neurosci. Res.51, 218.Li, Z., et al. 1996. J. Med. Chem.39, 4089.Saatman, K.E, et al. 1996. Proc. Natl. Acad. Sci. USA93, 3428.Bartus, R.T., et al. 1995. Neurol. Res.17, 249.Bartus, R.T., et al. 1994. Stroke25, 2265.

Packaging

1, 5 mg in Plastic ampoule

Packaged under inert gas

Physical form

Supplied as a trifluoroacetate salt.

Reconstitution

Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Sequence

Z-Leu-Abu-CONH(CH₂)₃-morpholine (Abu = A-aminobutyric acid)

Warning

Toxicity: Standard Handling (A)