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. Packaging 1 mg in Plastic ampoule 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.