Biochem/physiol Actions

Reversible: yes

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

Product does not compete with ATP.

Cell permeable: yes

Primary TargetAkt1, Akt2, Akt3

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.

Legal Information

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

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.

Packaging

1 mg in Plastic ampoule

Packaged under inert gas

Please refer to vial label for lot-specific concentration.

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).

Warning

Toxicity: Irritant (B)