Biochem/physiol Actions

Target IC₅₀: 625 nM in blocking Akt-mediated FOXO1a nuclear export; ﹤1.25 µM in blocking Akt-mediated cell proliferation in 786-O cells

Reversible: yes

Product does not compete with ATP.

Primary TargetAkt

Cell permeable: yes

General description

A cell permeable and reversible benzimidazole compound that inhibits Akt phosphorylation/activation by targeting the ATP binding site of a kinase upstream of Akt, but downstream of PI 3-K. Shown to block Akt-mediated FOXO1a nuclear export (IC_{50﹤/SUB> = 625 nM) and cell proliferation (IC50﹤/SUB><1.25 M) in 786-O cells. Unlike phosphatidylinositol analog-based Akt inhibitors (Cat. Nos. 124005, 124008, 124009), this inhibitor does not affect PI3K. A 10 mM (1 mg/163 l) solution of Akt Inhibitor IV in DMSO is also available.}

A cell-permeable and reversible benzimidazole compound that inhibits Akt phosphorylation/activation presumably by targeting the ATP binding site of a kinase upstream of Akt, but downstream of PI3-K. Shown to block Akt-mediated FOXO1a nuclear export (IC_{50﹤/sub> = 625 nM) and cell proliferation (IC50﹤/sub><1.25 µM) in 786-O cells. Unlike phosphatidylinositol analog-based Akt inhibitors (Cat. Nos. 124005, 124008, 124009), this inhibitor does not affect PI3-K.}

Legal Information

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

Other Notes

Kau, T.R., et al. 2003. Cancer Cell4, 463.Selected CitationsLee, J., et al. 2009. Cell Stem Cell5, 76.

Packaging

Packaged under inert gas

1 mg in Glass bottle

5 mg in Plastic ampoule

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)