Binucleine 2
目录号 : GC42933An inhibitor of Drosophila Aurora B kinase
Cas No.:220088-42-6
Sample solution is provided at 25 µL, 10mM.
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Binucleine 2 is an isoform-specific and ATP-competitive inhibitor of Drosophila Aurora B kinase (Ki = 0.36 µM), a kinase involved in cell division. It is specific for Drosophila Aurora B kinase, inhibiting it in a dose-dependent manner, with minimal inhibition of human or X. laevis Aurora B kinases at concentrations up to 100 µM. Binucleine 2 induces mitotic and cytokinesis defects in Drosophila Kc167 cells. It prevents Drosophila S2 cells from assembling a contractile ring during cell division when used at a concentration of 40 µM but does not affect ring ingression, suggesting that Aurora B kinase activity is not required for that step.
Cas No. | 220088-42-6 | SDF | |
Canonical SMILES | CN(C)/C=N/C1=C(C#N)C=NN1C2=CC=C(F)C(Cl)=C2 | ||
分子式 | C13H11ClFN5 | 分子量 | 291.7 |
溶解度 | Chloroform: Slightly Soluble,DMSO: Slightly Soluble | 储存条件 | Store at -20°C |
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1 mg | 5 mg | 10 mg | |
1 mM | 3.4282 mL | 17.1409 mL | 34.2818 mL |
5 mM | 0.6856 mL | 3.4282 mL | 6.8564 mL |
10 mM | 0.3428 mL | 1.7141 mL | 3.4282 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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Binucleine 2, an isoform-specific inhibitor of Drosophila Aurora B kinase, provides insights into the mechanism of cytokinesis
ACS Chem Biol 2010 Nov 19;5(11):1015-20.PMID:20804174DOI:PMC3039078
Aurora kinases are key regulators of cell division and important targets for cancer therapy. We report that Binucleine 2 is a highly isoform-specific inhibitor of Drosophila Aurora B kinase, and we identify a single residue within the kinase active site that confers specificity for Aurora B. Using Binucleine 2, we show that Aurora B kinase activity is not required during contractile ring ingression, providing insight into the mechanism of cytokinesis.