208743

Calpain Inhibitor XI

The Calpain Inhibitor XI, also referenced under CAS 145731-49-3, controls the biological activity of Calpain. This small molecule/inhibitor is primarily used for Protease Inhibitors applications.

• Synonym(e): Calpain Inhibitor XI, Z-L-Abu-CONH(CH₂)₃-morpholine
• Empirische Formel (Hill-System): C₂₆H₄₀N₄O₆
• CAS-Nummer: 145731-49-3
• Molekulargewicht: 504.62
• UNSPSC-Code: 12352200
• NACRES: NA.77

Eigenschaften

• Qualitätsniveau: 100
• Assay: ≥95% (HPLC)
• Form: solid
• Hersteller/Markenname: Calbiochem^®
• Lagerbedingungen: OK to freeze; desiccated (hygroscopic)
• Farbe: white to off-white
• Löslichkeit: DMSO: 5 mg/mL
• Versandbedingung: ambient
• Lagertemp.: 2-8°C

Beschreibung

Allgemeine Beschreibung

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.

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.

Biochem./physiol. Wirkung

Cell permeable: yes

Primary Target
calpain 1, calpain 2

Product does not compete with ATP.

Reversible: yes

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

Verpackung

Packaged under inert gas

Warnhinweis

Toxicity: Standard Handling (A)

Sequenz

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

Physikalische Form

Supplied as a trifluoroacetate salt.

Rekonstituierung

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

Sonstige Hinweise

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.

Rechtliche Hinweise

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

Sicherheitshinweise

• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 1
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable