| 名称 | Hesperadin |
| 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. |
| 细胞实验 | HeLa cells and PtK1 cells are added Hesperadin 500 nM for 24 and 48 hours. |
| 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. |
| 体外活性 | 在HeLa细胞中，Hesperadin通过抑制Aurora B的功能，干扰染色体连接，造成有丝分裂和细胞质分裂缺陷，导致细胞增殖停止和多倍体化。Hesperadin在20-100 nM浓度作用下，导致有丝分裂活化组蛋白H3在Ser10位点的磷酸化丢失。当Hesperadin浓度达到1 μM时，其他激酶（AMPK, Lck, MKK1, MAPKAP-K1, CHK1, 和 PHK）活性显著降低。在体外激酶测定中，Hesperadin（IC50 = 40 nM）阻断了来自病原性锥虫（Trypanosoma brucei）的TbAUK1（T. brucei Aurora kinase-1）对重组色质组蛋白H3的磷酸化。Hesperadin（IC50 = 48 nM）显著抑制了培养的传染性血液形式（BF）细胞的生长，而以IC50 = 550 nM的浓度弱抑制了昆虫循环阶段（PF）细胞的生长。 |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (3.87 mM), Sonication is recommended.
DMSO : 55.3 mg/mL (107.04 mM), Sonication is recommended.
Ethanol : 27.7 mg/mL (53.61 mM), Sonication is recommended.
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| 关键字 | TbAUK1 | procyclic | Parasite | Inhibitor | inhibit | InfluenzaVirus | Influenza Virus | Hesperadin | forms | bloodstream | Autophagy | AuroraKinase | Aurora Kinase | Aurora B (human) | Aurora |
| 相关产品 | 2-Amino-2-methyl-1-propanol | Guanidine hydrochloride | Naringin | Aceglutamide | Fenpyroximate | Alginic acid | Doxycycline | Metronidazole | Hemin | Hydroxychloroquine | Stavudine | Paeonol |
| 相关库 | 抑制剂库 | 经典已知活性库 | 已知活性化合物库 | 细胞周期化合物库 | 自噬库 | 激酶抑制剂库 | 抗衰老化合物库 | NO PAINS 化合物库 | 抗病毒库 | 抗寄生虫库 | 膜蛋白靶向化合物库 | 共价抑制剂库 |