General 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 µM, respectively) in a reversible, ATP-uncompetitive (K_i = 3.36 µM), and MT-noncompetitive (K_i = 1.6 µM) manner, with little effect against the ATPase activity of 12 other kinesins (≤20% inhibition at 50 µM), 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 µM 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.

Legal Information

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

Other Notes

Tcherniuk, S., et al. 2010. Angew. Chem. Int. Ed.49, 8228.

Packaging

25 mg in Glass bottle

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: Regulatory Review (Z)