Kinesore

• CAT Number: I019809
• CAS Number: 363571-83-9
• Molecular Formula: C20H16Br2N4O4
• Molecular Weight: 536.17
• Purity: ≥95%
• Synonyms: 3,5-dibromo-N-[(E)-[2,5-dimethyl-1-(3-nitrophenyl)pyrrol-3-yl]methylideneamino]-4-hydroxybenzamide
• InChI: InChI=1S/C20H16Br2N4O4/c1-11-6-14(12(2)25(11)15-4-3-5-16(9-15)26(29)30)10-23-24-20(28)13-7-17(21)19(27)18(22)8-13/h3-10,27H,1-2H3,(H,24,28)/b23-10+
• InChIKey: DUGCMEGLYHBMAR-AUEPDCJTSA-N
• SMILES: CC1=CC(=C(N1C2=CC(=CC=C2)[N+](=O)[O-])C)C=NNC(=O)C3=CC(=C(C(=C3)Br)O)Br

Kinesore is an inhibitor of the KLC2-SKIP Interaction.
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].

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.
 [Content Brief]