INSOLUTION AKT INHIBITOR VIII ISOZYME-SELECTIVE AKTI-1/2 - CALBIOCHEM

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

Molecular Weight: 551.64. Empirical Formula: C₃₄H₂₉N₇O. 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. Storage Class Code: 10 - Combustible liquids. WGK: WGK 2. Flash Point(F): 188.6 °F - (Dimethylsulfoxide). Flash Point(C): 87 °C - (Dimethylsulfoxide).