A reversible Kif18A inhibitor
BTB-1 is a reversible inhibitor of the kinesin-8 family motor protein Kif18A (IC50 = 1.69 μM).1 It is selective for Kif18A over a panel of seven kinesins at 100 μM. BTB-1 (100 μM) inhibits Kif18A-dependent microtubule motility in a microtubule gliding assay. It induces mitotic accumulation of HeLa cells in a dose-dependent manner.
1.Catarinella, M., Grüner, T., Strittmatter, T., et al.BTB-1: A small molecule inhibitor of the mitotic motor protein Kif18AAngew. Chem. Int. Ed. Engl.48(48)9072-9076(2009)
Kinase experiment: | BTB-1 is prepared in DMSO. The activity of His-Kif18Amotor at increasing concentrations of ATP is monitored in the presence of 3 μM Mts and increasing concentrations of BTB-1 (0.21 μM, 0.42 μM, 0.85 μM, 1.7 μM) or DMSO as control[1]. |
参考文献: [1]. Catarinella M, et al. BTB-1: a small molecule inhibitor of the mitotic motor protein Kif18A. Angew Chem Int Ed Engl. 2009;48(48):9072-6. | |
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