Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Hesperadin 是 Aurora A 和 B 的 ATP 竞争性吲哚酮抑制剂,抑制 Aurora B 的 IC50值为250nM。它通过阻断核分裂和胞质分裂而抑制布鲁氏锥虫的生长。它也是一种广谱流感抗病毒剂。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 292 | 现货 | ||
2 mg | ¥ 413 | 现货 | ||
5 mg | ¥ 663 | 现货 | ||
10 mg | ¥ 1,230 | 现货 | ||
25 mg | ¥ 2,460 | 现货 | ||
50 mg | ¥ 3,670 | 现货 | ||
100 mg | ¥ 5,290 | 待询 | ||
1 mL * 10 mM (in DMSO) | ¥ 753 | 现货 |
产品描述 | Hesperadin(IC50=250 nM) effectively inhibits Aurora B. It potently reduces the activity of AMPK, MAPKAP-K1, MKK1, Lck, CHK1 and PHK, but it could not inhibit MKK1 activity in vivo. |
靶点活性 | Aurora B:250 nM |
体外活性 | In HeLa cells, Hesperadin causing defects in mitosis and cytoplasmic division, leading to cell proliferation and polyploidization stopped, because of Aurora B function inhibition during chromosome connection. Addition of 20-100 nM Hesperadin leading to loss of phosphorylation of the mitogenic histone H3 at the Ser10 site. When Hesperadin concentration was 1 μM, other kinases (AMPK, Lck, MKK1, MAPKAP-K1, CHK1, and PHK) activity were significantly reduced.In an in vitro kinase assay, Hesperadin (IC50 = 40 nM) blocked recombinant trypton histone H3 phosphorylation by T. brucei Aurora kinase-1 (TbAUK1) from the pathogenic Trypanosoma brucei. Hesperadin (IC50 = 48 nM) significantly inhibited the growth of cultured infectious blood form (BF) cells, while Hesperadin (IC50 = 550 nM) and weakly inhibited the growth of insect circulation stage (PF) cells. |
激酶实验 | For the Aurora B kinase assay, HeLa cells are lysed in a buffer containing 50 mM NaCl, then centrifuging at 13,000 rpm for 20 minutes at 4 °C. Discard supernatant, add 15 mL lysis buffer containing 250 mM NaCl in order to obtain active Aurora B kinase. Centrifuging at low-speed supernatant of the latter extract is used for immunoprecipitation. Monoclonal mouse anti–AIM-1, or mouse anti-HA, is coupled to GammaBind Plus Sepharose, and beads are rotated over-end in the extract for 90 minutes at 4 °C. Beads are washed, aliquoted, and washed in kinase buffer (20 mM Tris, pH 7.5, 150 mM NaCl, 10 mM MgCl2, 1 mM DTT, 10 mM NaF). The kinase assay is performed with 10 μL beads in 20 μL kinase buffer containing 5 μg histone H3, 10 μM ATP, 2.5 μCi [γ-32P]ATP, and different concentrations of Hesperadin for 20 minutes at 37 °C. |
细胞实验 | HeLa cells and PtK1 cells are added Hesperadin 500 nM for 24 and 48 hours. |
分子量 | 516.65 |
分子式 | C29H32N4O3S |
CAS No. | 422513-13-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 55.3 mg/mL (100 mM)
Ethanol: 27.7 mg/mL (50 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 1.9355 mL | 9.6777 mL | 19.3555 mL | 48.3887 mL |
5 mM | 0.3871 mL | 1.9355 mL | 3.8711 mL | 9.6777 mL | |
10 mM | 0.1936 mL | 0.9678 mL | 1.9355 mL | 4.8389 mL | |
20 mM | 0.0968 mL | 0.4839 mL | 0.9678 mL | 2.4194 mL | |
50 mM | 0.0387 mL | 0.1936 mL | 0.3871 mL | 0.9678 mL | |
DMSO | 100 mM | 0.0194 mL | 0.0968 mL | 0.1936 mL | 0.4839 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Hesperadin 422513-13-1 Autophagy Cell Cycle/Checkpoint Chromatin/Epigenetic Microbiology/Virology Influenza Virus Parasite Aurora Kinase Aurora procyclic forms bloodstream inhibit Inhibitor inhibitor