Polo-like Kinase Inhibitor II, BTO-1

Toxicity: Harmful (C)

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.

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.

Packaged under inert gas

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

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