Polo-like Kinase Inhibitor II, BTO-1

A cell-permeable benzothiazolo-N-oxide compound that targets the ATP-binding pocket of polo-like kinase and is shown to inhibit Plk1 kinase activity in cell-free kinase assays (IC₅₀ = 8.0 µM) and suppress the phosphorylation of cellular Plk1 substrate Cdc25C in rat kangaroo kidney-derived PTK cells (75% inhibition at 6.3 µM). BTO-1 treatment of cultured cells results in mitosis defects consistent with loss-of-Plk1 phenotypes seen in Plk1 RNAi-treated U20S cells, including the appearance of monopolar spindles and the reduction of γ-tubulin at the centrosomes. Plk1 inhibition by BTO-1 in HeLa cells results in a blockage of Rho and Rho-GEF recruitment, which is essential for the assembly of a functional contractile ring.

Packaged under inert gas

Toxicity: Harmful (C)

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

Brennan, I.M., et al. 2007. PloS ONE2, e409.
Peters, U., et al. 2006. Nat. Chem. Biol.2, 618.
McInnes, C., et al. 2006. Nat. Chem. Biol.2, 608.

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