BTB-1

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Chemical Structure| 86030-08-2 同义名 : NSC 156750;NSC 658180
CAS号 : 86030-08-2
货号 : A276415
分子式 : C12H8ClNO4S
纯度 : 99%
分子量 : 297.714
MDL号 : MFCD00052250
存储条件：

Pure form Sealed in dry,Room Temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(352.69 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Kif18A is a mitotic motor protein essential for the correct alignment of chromosomes at the spindle equator. BTB1 potently inhibits the ATPase activity of Kif18A with an IC50 value of 1.69μM. The re-synthesized BTB1 inhibited His-Kif18Amotor with equal potency (IC50=1.86μM). The flushing in of 100μM BTB1 almost completely inhibited His-Kif18AFL-dependent microtubule motility. After the wash-out of BTB1, His-Kif18AFL regained most of its activity. The ATPase activity of His-Kif18Amotor was not affected by BTB1(100μM) in the absence of microtubules. BTB1 significantly inhibited microtubule-stimulated ATPase activity of His-Kif18Amotor as compared to the DMSO-treated group. Incubation of HeLa cells with BTB1 (30 and 40μM) for 18h induced the accumulation of cells in mitosis[3].
作用机制 BTB1 is a potent and selective Kif18A inhibitor that reversibly inhibits the motility of Kif18A in an ATP-competitive manner[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.36mL

0.67mL

0.34mL

16.79mL

3.36mL

1.68mL

33.59mL

6.72mL

3.36mL
参考文献

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

[2]Catarinella M, Gruner T, et al. BTB-1: a small molecule inhibitor of the mitotic motor protein Kif18A. Angew Chem Int Ed Engl. 2009;48(48):9072-6.

[3]Catarinella M, Grüner T, Strittmatter T, Marx A, Mayer TU. BTB-1: a small molecule inhibitor of the mitotic motor protein Kif18A. Angew Chem Int Ed Engl. 2009;48(48):9072-9076. doi:10.1002/anie.200904510