Kinesore

Research use only, not for human use.

Kinesore is a small molecule activator of kinesin-1 that inhibits KLC2-SKIP interaction with IC50 of 101 uM, Ki of 49 uM.

Kinesore is a small molecule activator of kinesin-1 that inhibits KLC2-SKIP interaction with IC50 of 101 uM, Ki of 49 uM; inhibits kinesin-1 interactions with short linear peptide motifs found in organelle-specific cargo adaptors, yet activates kinesin-1's function of controlling microtubule dynamics in cells; induces the remodeling of the microtubule network.

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.

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Kinesore

Cytoskeleton/Cell Adhesion Molecules

Kinesin

Kinesin

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363571-83-9

536.18

C20H16Br2N4O4

>98% (HPLC)

DMSO : 125 mg/mL 233.14 mM

O=C(N/N=C/C1=C(C)N(C2=CC=CC([N+]([O-])=O)=C2)C(C)=C1)C3=CC(Br)=C(O)C(Br)=C3

(E)-3,5-Dibromo-N'-((2,5-dimethyl-1-(3-nitrophenyl)-1H-pyrrol-3-yl)methylene)-4-hydroxybenzohydrazide

(-20℃)

With Ice Pack

≥ 2 years