Akt Inhibitor VIII; Isozyme-Selective; Akti-1/2

Biochem/physiol Actions

Reversible: yes

Product does not compete with ATP.

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

Cell permeable: yes

Primary TargetAkt1, Akt2, Akt3

General description

A cell-permeable and reversible quinoxaline compound that potently and selectively inhibits 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 appears 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. A 10 mM (1 mg/181 µl) solution of Akt Inhibitor VIII, Isozyme-Selective, Akti-1/2 (Cat. No. 124017) in DMSO is also available.

A cell-permeable, reversible, 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

Calleja, V., et al. 2009. PLoS Biol.7, e17.Logie, L., et al. 2007. Diabetes56, 228.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

5 mg in Glass bottle

Packaged under inert gas

Reconstitution

Following reconstitution, aliquot and freeze (-70°C). Stock solutions are stable for up to 6 months at -70°C.

Warning

Toxicity: Standard Handling (A)