General description

A cell-permeable indolinone compound that acts as a potent, ATP site-targeting PDK1 inhibitor (IC₅₀ = 6 nM) and effectively suppresses cellular Akt Thr³⁰⁸ phosphorylation level in PC-3 cultures (IC₅₀ ≤1 µM), while affecting PKA (IC₅₀ = 1.6 µM) and 7 other kinases (IC₅₀ ≥600 nM) only at much higher concentrations. Its in vivo applicability is limited by a low aqueous solubility (2 µg/ml in PBS) and poor pharmacokinetics.

Legal Information

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

Other Notes

Islam, I., et al. 2007. Bioorg. Med. Chem. Lett.17, 3819.Islam, I., et al. 2007. Bioorg. Med. Chem. Lett.17, 3814.

Packaging

Packaged under inert gas

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)