BTB-1

A reversible Kif18A inhibitor

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库存: 现货

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数量
5mg

￥700.00

560.00

- +
10mg

￥950.00

760.00

- +
50mg

￥3112.00

2490.00

- +
100mg

￥5450.00

4360.00

- +

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Background

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)

Protocol

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.
[2]. Braun J, et al. Synthesis and biological evaluation of optimized inhibitors of the mitotic kinesin Kif18A. ACS Chem Biol. 2015 Feb 20;10(2):554-60.