General description

A cell-permeable aminopyrimidine compound that acts as a potent, ATP-competitive and reversible multi-kinase inhibitor (IC₅₀ = 11 nM for PDK1 at ≤ 10 µM of ATP; IC₅₀ = 5 , 6, 19, 31, 41 and 111 nM for NUAK1, TBK1, MARK4, Aurora B, IKKε and PDK1 at 100 µM of ATP, respectively) and displays 50-fold greater selectivity over Cdk2/E, EGFR, GSK-3β, IR, c-Kit, PKA, PKC, TAK1 and VEGFR. Shown to block PDK1/Akt signaling, induce growth arrest and apoptosis in PC-3 and MDA-468 cells (IC₅₀ = 0.25 and 0.75 µM, respectively); further, inhibit phosphorylation (pSer³⁹⁶), nuclear translocation and transcriptional activity of IRF3 and reduce IFN-β production in stimulated macrophages.

Legal Information

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

Other Notes

Clark, K., et al. 2009. J. Biol. Chem.284, 14136.Tamgumcy, T., et al. 2008. Exp. Cell Res.314, 2299.Feldman, R.I., et al. 2005. J. Biol. Chem.280, 19867.

Packaging

Packaged under inert gas

10 mg in Glass bottle

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Warning

Toxicity: Standard Handling (A)