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513022

Sigma-Aldrich

PD 150606

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

Synonyme(s) :

PD 150606, 3-(4-Iodophenyl)-2-mercapto-(Z)-2-propenoic Acid

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About This Item

Formule empirique (notation de Hill):
C9H7IO2S
Numéro CAS:
426821-41-2
Poids moléculaire :
306.12
Code UNSPSC :
12352200
Nomenclature NACRES :
NA.77

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 générale

A cell-permeable, non-competitive, selective non-peptide calpain inhibitor [Ki = 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 (Ki = 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 Ki: 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

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

Certificats d'analyse (COA)

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Mehmet Şerif Aydın et al.
iScience, 26(10), 107715-107715 (2023-09-13)
Trauma, vascular events, or neurodegenerative processes can lead to axonal injury and eventual transection (axotomy). Neurons can survive axotomy, yet the underlying mechanisms are not fully understood. Excessive water entry into injured neurons poses a particular risk due to swelling

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