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Description

A cell-permeable acrylonitrile compound that inhibits the kinesin-6 family member MKLP-2 (Mitotic kinesin-like protein 2, IC50 against basal and microtubule-/MT-stimulated ATPase activity = 1.35 and 0.83 microM, respectively) in a reversible, ATP-uncompetitive (Ki = 3.36 microM), and MT-noncompetitive (Ki = 1.6 microM) manner, with little effect against the ATPase activity of 12 other kinesins (&le,20% inhibition at 50 microM), including the close related MKLP-1 and MPP1 (M-phase phosphoprotein 1). Shown to inhibit cellular Aurora B and Survivin anaphase centromere-to-spindle midzone relocation in HeLa cultures (50 microM for 8 h), but not MKLP-1- or Kif4-mediated PRC1 relocation, resulting in misaligned chromosomes (70% of total metaphase cells), multipolar spindles (14% of total metaphase cells), and eventual apoptosis.