A cell-permeable vanillin-derived pyridyl-ethanamine compound that acts as a highly potent type II Plk1 inhibitor (IC₅₀ of 200 pM) and targets the less conserved DFG motif that is only accessible when the kinase is in its inactive DFG-out conformation, resulting in an excellent selectivity over Plk2 (IC₅₀ >66 µM), Plk3 (IC₅₀ = 875 nM), and aurora A kinase (no detectable effect). Shown to inhibit the proliferation of HeLa cells with an EC₅₀ of 18 µM.

Packaged under inert gas

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

Keppner, S., et al. 2009. ChemMedChem.4, 1806.

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

Toxicity: Standard Handling (A)