124017

Akt Inhibitor VIII, Akti-1/2

InSolution, ≥95%, Isozyme-Selective

• Synonyme(s) : InSolution Akt Inhibitor VIII, Isozyme-Selective, Akti-1/2
• Formule empirique (notation de Hill): C₃₄H₂₉N₇O
• Poids moléculaire : 551.64
• Code UNSPSC : 12352200

Propriétés

• Niveau de qualité: 100
• Pureté: ≥95% (HPLC)
• Forme: liquid
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; desiccated (hygroscopic); protect from light
• Conditions d'expédition: wet ice
• Température de stockage: −70°C

Description

Description générale

A cell-permeable, potent, and selective inhibitor of Akt1/Akt2 activity (IC₅₀ = 58 nM, 210 nM, and 2.12 µM for Akt1, Akt2, and Akt3, respectively, in in vitro kinase assays). The inhibition is reported to be pleckstrin homology (PH) domain-dependent. It does not exhibit any inhibitory effect against PH domain-lacking Akts, or other closely related AGC family kinases, PKA, PKC, and SGK, even at concentrations as high as 50 µM. Overcomes Akt1/Akt2-mediated resistance to chemotherapeutics in tumor cells and is shown to block basal and stimulated phosphorylation/activation of Akt1/Akt2 both in cultured cells in vitro and in mice in vivo.

Actions biochimiques/physiologiques

Cell permeable: yes

Primary Target
Akt1, Akt2, Akt3

Product does not compete with ATP.

Reversible: yes

Target IC₅₀: 58 nM, 210 nM, and 2.12 µM for Akt1, Akt2, and Akt3, respectively, in in vitro kinase assays

Conditionnement

Packaged under inert gas

Please refer to vial label for lot-specific concentration.

Avertissement

Toxicity: Irritant (B)

Forme physique

A 10 mM (1 mg/181 µl) solution of Akt Inhibitor VIII, Isozyme-Selective, Akti-1/2 (Cat. No. 124018) in DMSO.

Reconstitution

Following initial thaw, aliquot and freeze (-70°C).

Autres remarques

Barnett, S.F., et al. 2005. Biochem. J.385, 399.
DeFeo-Jones, D., et al. 2005. Mol. Cancer Ther.4, 271.
Zhao, Z., et al. 2005. Bioorg. Med. Chem. Lett.15, 905.
Lindsley, C.W., et al. 2005. Bioorg. Med. Chem. Lett.15, 761.

Informations légales

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

Informations sur la sécurité

• Code de la classe de stockage: 10 - Combustible liquids
• Classe de danger pour l'eau (WGK): WGK 2
• Point d'éclair (°F): 188.6 °F - (Dimethylsulfoxide)
• Point d'éclair (°C): 87 °C - (Dimethylsulfoxide)