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Monastrol is a reversible, cell-permeable inhibitor of the motor protein Eg5 (kinesin family protein 11, Kif11), blocking basal ATPase activity in vitro (IC50 = 6.1 µM) and inducing the formation of monoastral spindles in cell-based assays (IC50 = 51.3 μM).. It arrests cells in mitosis without targeting tubulin and, as a result, does not interfere with microtubule dependent processes. Monastrol induces activation of the spindle assembly checkpoint and the resulting mitotic arrest can lead to cell death in certain tumor cell lines. |