General description

A cell-permeable naphthyridinone compound that acts as an allosteric Akt1/2-selective inhibitor (IC₅₀ = 3.5, 42, and 1900 nM against Akt1, Akt2, and Akt3, respectively) in a PH domain-dependent, but not ATP-competitive, manner, with little activity against a panel of more than 160 other kinases, including the related AGC family kinases (inactive at 10 µM against GSK, PDK1, PKA, PKC, and SGK). Effectively inhibits the basal Akt phosphorylation in cancer cells with deregulated Akt pathway activation, including the HCT116 colorectal carcinoma and a panel of breast cancer cell lines (IC₅₀﹤500 nM), and suppresses Akt-dependent cell growth both in cultures in vitro (IC₅₀ ≤1 µM) and in mice in vivo (50 to 100 mg/kg, SC). Although also referred to as AKTi-1/2, this is not the same compound as Akt Inhibitor XV (Cat. Nos. 124017 & 124018).

A cell-permeable naphthyridinone compound that acts as an allosteric Akt1/2-selective inhibitor (IC₅₀ = 3.5, 42, and 1900 nM against Akt1, Akt2, and Akt3, respectively) in a PH domain-dependent, but not ATP-competitive, manner, with little activity against a panel of more than 160 other kinases, including the related AGC family kinases (inactive at 10 M against GSK, PDK1, PKA, PKC, and SGK). Effectively inhibits the basal Akt phosphorylation in cancer cells with deregulated Akt pathway activation, including the HCT116 colorectal carcinoma and a panel of breast cancer cell lines (IC₅₀﹤500 nM), and suppresses Akt-dependent cell growth both in cultures in vitro (IC₅₀ ≤1 M) and in mice in vivo (50 to 100 mg/kg, SC). Although also referred to as AKTi-1/2, this is not the same compound as Akt Inhibitor XV.

Legal Information

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

Other Notes

She, Q.B., et al. 2010. Cancer Cell18, 39.Bilodeau, M.T., et al. 2008. Bioorg. Med. Chem. Lett.18, 3178.She, Q.B, et al. 2008. PLoS One3, e3065.

Packaging

2 mg in Glass bottle

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Warning

Toxicity: Standard Handling (A)