513022

PD 150606

A cell-permeable, non-competitive, selective non-peptide calpain inhibitor [K_i = 210 nM for calpain-1 and 370 nM for calpain-2.

• Synonyme(s) : PD 150606, 3-(4-Iodophenyl)-2-mercapto-(Z)-2-propenoic Acid
• Formule empirique (notation de Hill): C₉H₇IO₂S
• Numéro CAS: 426821-41-2
• Poids moléculaire : 306.12
• Code UNSPSC : 12352200
• Nomenclature NACRES : NA.77

Propriétés

• Niveau de qualité: 100
• Pureté: ≥95% (HPLC)
• Forme: solid
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: off-white
• Solubilité: DMSO: 100 mg/mL; methanol: 25 mg/mL
• Conditions d'expédition: ambient
• Température de stockage: −20°C

Description

Description générale

A cell-permeable, non-competitive, selective non-peptide calpain inhibitor [K_i = 210 nM for calpain-1 (Cat. Nos. 208712 and 208713) and 370 nM for calpain-2 (Cat. Nos. 208715 and 208718)] directed towards the calcium binding sites of calpain. Exhibits high specificity for calpains relative to other proteases, such as cathepsin B and cathepsin L. Does not shield calpain against inactivation by the active-site inhibitor trans-(epoxysuccinyl)-L-leucyl-amido-3-methylbutane. Reportedly prevents dexamethasone-induced apoptosis in thymocytes.

A cell-permeable, selective non-peptide calpain inhibitor (K_i = 210 nM for calpain I and 370 nM for calpain II) directed towards the calcium- binding sites of calpain. Exhibits high specificity for calpains relative to other proteases, such as cathepsin B and L. PD 150606 is a non-competitive inhibitor with respect to the substrate and does not shield calpain against inactivation by the active-site inhibitor trans-(epoxysuccinyl)-L-leucyl-amido-3-methylbutane. Reportedly prevents dexamethasone-induced apoptosis of thymocytes.

Actions biochimiques/physiologiques

Cell permeable: yes

Primary Target
Calpain-1

Product does not compete with ATP.

Reversible: no

Target K_i: 210 nM for calpain-1 and 370 nM for calpain-2

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.

Autres remarques

Lin, G.D., et al. 1997. Nat. Struct. Biol. 4, 539.
Squier, M.K., and Cohen, J.J. 1997. J. Immunol. 158, 3960.
Edelstein, C.L., et al. 1996. Kidney Int. 50, 1150.
Wang, K.K.W., et al. 1996. Proc. Natl. Acad. Sci. USA 93, 6687.

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 1
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable