| Bioactivity | Kinesore is an inhibitor of the KLC2-SKIP Interaction. | ||||||||||||
| Target | KLC2-SKIP. | ||||||||||||
| Invitro | Remarkably, in kinesore-treated cells, the microtubule network is entirely reorganized into a series of loops and bundles. In addition, the lysosomal compartment accumulates in a juxtanuclear position, where there are relatively few microtubules. At 50 μM kinesore, this phenotype is highly penetrant, with 95±2.4% (n=3, total of 200 cells) of cells exhibiting a reorganized nonradial microtubule network. In titration experiments, in cells treated for 1 h, this phenotype becomes apparent at a concentration of 25 μM kinesore, with relatively little effect at or below concentrations of 12.5 μM. The effect is reversible because a 2-h washout of kinesore from cells treated for 1 h led to the reestablishment of the radial microtubule array. This kinesore-induced reorganization of the microtubule network is observed in a panel of mammalian normal and cancer cell lines. In wild-type cells, 50 μM kinesore induces the remodeling of the microtubule network and the formation of extensive microtubule-rich projections. This phenotype is strongly suppressed in Kif5B knockout cells, confirming that microtubule remodeling induced by kinesore is dependent upon the presence of kinesin-1[1]. | ||||||||||||
| Name | Kinesore | ||||||||||||
| CAS | 363571-83-9 | ||||||||||||
| Formula | C20H16Br2N4O4 | ||||||||||||
| Molar Mass | 536.17 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Randall TS, et al. A small-molecule activator of kinesin-1 drives remodeling of the microtubule network. Proc Natl Acad Sci U S A. 2017 Dec 26;114(52):13738-13743. |