124017

Akt Inhibitor VIII, Akti-1/2

InSolution, ≥95%, Isozyme-Selective

• Synonym(s): InSolution Akt Inhibitor VIII, Isozyme-Selective, Akti-1/2
• Empirical Formula (Hill Notation): C₃₄H₂₉N₇O
• Molecular Weight: 551.64
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Quality Level: 100
• assay: ≥95% (HPLC)
• form: liquid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; desiccated (hygroscopic); protect from light
• shipped in: wet ice
• storage temp.: −70°C

Description

General description

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.

Biochem/physiol Actions

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

Packaging

Packaged under inert gas

Please refer to vial label for lot-specific concentration.

Warning

Toxicity: Irritant (B)

Physical form

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).

Other Notes

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.

Legal Information

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

Safety Information

• Storage Class: 10 - Combustible liquids
• wgk_germany: WGK 2
• flash_point_f: 188.6 °F - closed cup - (Dimethylsulfoxide)
• flash_point_c: 87 °C - closed cup - (Dimethylsulfoxide)