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Key Documents

208733

Sigma-Aldrich

Calpain Inhibitor Set

The Calpain Inhibitor Set controls the biological activity of Calpain. This small molecule/inhibitor is primarily used for Protease Inhibitors applications.

Synonyme(s) :

Calplain inhibitor

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About This Item

Code UNSPSC :
12352200
Nomenclature NACRES :
NA.77

Niveau de qualité

Forme

solid

Puissance

8 nM Ki

Fabricant/nom de marque

Calbiochem®

Conditions de stockage

OK to freeze
desiccated
protect from light

Conditions d'expédition

ambient

Température de stockage

−20°C

Description générale

Calpains are a family of calcium-dependent thiol-proteases that act on a wide variety of cytoskeletal, membrane-associated, and regulatory proteins. There are two major isoforms: calpain I (µ-form) and calpain II (m-form), which differ in their calcium requirement for activation Calpains are composed of heterodimers of 80 kDa and a 30 kDa subunits. The 80 kDa unit has the catalytic site and is unique to each isozyme, whereas the 30 kDa unit is the regulatory subunit and is common to both µ- and m-isozymes.



More recently, attention has been focused on the pathological significance of calcium accumulation in the central nervous system following cerebral ischemia and traumatic brain injury. Over-activation of NMDA, kainate, and AMPA receptors in the brain leads to sustained influx of Ca2+ through the voltage-gated calcium channels. Overexpression of calpains has been positively linked to both acute and chronic neurodegenerative processes including ischemia, trauma, and Alzheimer′s disease. In Alzheimer′s disease the ratio of active (76 kDa) to inactive (80 kDa) µ-calpain is reported to be much higher Calpain-dependent proteolysis is usually the late-stage common pathway towards cell death induced by excitotoxic compounds, hence, a selective inhibition of calpains to limit neuronal damage appears to be a viable therapeutic measure.
Contains 5 mg of ALLN (Cat. No. 208719), 25 mg of Calpain Inhibitor III (Cat. No. 208722), 5 mg of Calpeptin (Cat. No. 03-34-0051), 1 mg of EST (Cat. No. 330005), and 5 mg of PD 150606 (Cat. No. 513022).

Actions biochimiques/physiologiques

Cell permeable: yes
Primary Target
calpain 1, calpain 2
Reversible: no

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Multiple Toxicity Values, refer to MSDS (O)

Autres remarques

Johnson, G.V.W., and Guttmann, R.P. 1997. BioEssays19, 1011.
Kampfl, A., et al. 1997. J. Neurotauma14, 121.
Sorimachi, H., et al., 1997. Biochem. J.328, 721.
Bartus, R.T., et al. 1995. Neurol. Res.17, 249.
Wang, K.K.W., and Yuen, P-W. 1994. Trends Pharmacol. Sci.15, 412.
Saito, K., et al. 1993. Proc. Natl. Acad. Sci. USA90, 2628.
Goll, D.E., et al. 1992. BioEssays14, 549.

Informations légales

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

Code de la classe de stockage

11 - Combustible Solids


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