Monastrol is a potent, specific, allosteric and reversible mitotic kinesin Eg5 inhibitor with IC50 of 14 uM (microtubule motility inhibition).
Monastrol does not inhibit microtubule motility driven by conventional kinesin at 200 uM.
Monastrol inhibits both the basal and the microtubule-stimulated ATPase activity of the Eg5 motor domain, does not compete with ATP binding to Eg5; arrests cells in mitosis with monoastral spindles.
(S)-monastrol is a more potent inhibitor of Eg5 activity in vitro and in vivo.
