Eg5-I

The Uses of Eg5-I

Eg5-I is a potent inhibitor of Eg5 affecting the mitosis process. Prevents the motor protein Eg5 (KSP) from establishing bipolar spindle during mitosis.

Biological Activity

eg5-i is a potent inhibitor of eg5.the kinesin-like spindle protein eg5, also known as ksp and kif11, is a motor protein that is essential for establishing a bipolar spindle during mitosis.

in vitro

previous study found that the interphase microtubule morphology was normal after the treatment of eg5-i, whereas spindle morphology mirrored that of the parent compound. eg5-i was tested for inhibitory activity against a selected panel of mitotic kinesins with no measurable inhibition detected. to determine whether eg5-i had a similar effect on ksp dynamics, cells were treated with eg5-i and probed for ksp localization with anti-ksp antibodies. eg5-i showed a dose-dependent depletion of ksp from the spindle, with a 1.63-fold increase in clearance of ksp over its parent compound, consistent with the biochemical-and cell-based assays. eg5-i blocked bipolar spindle formation, whereas the parent compound was weakly active. eg5-i was also evaluated for anti-proliferative activity against the nci60 tumor panel and the growth inhibitory concentration anged from 10 nm to 3 μm across the panel, respectively [1].

References

[1] rodriguez, d. ,ramesh, c.,henson, l.h., et al. synthesis and characterization of tritylthioethanamine derivatives with potent ksp inhibitory activity. bioorganic & medicinal chemistry 19(18), 5446-5453 (2011).