| 名稱 | 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. |
| 細(xì)胞實驗 | HeLa cells and PtK1 cells are added Hesperadin 500 nM for 24 and 48 hours. |
| 激酶實驗 | 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. |
| 體外活性 | 在HeLa細(xì)胞中，Hesperadin通過抑制Aurora B的功能，干擾染色體連接，造成有絲分裂和細(xì)胞質(zhì)分裂缺陷，導(dǎo)致細(xì)胞增殖停止和多倍體化。Hesperadin在20-100 nM濃度作用下，導(dǎo)致有絲分裂活化組蛋白H3在Ser10位點的磷酸化丟失。當(dāng)Hesperadin濃度達(dá)到1 μM時，其他激酶（AMPK, Lck, MKK1, MAPKAP-K1, CHK1, 和 PHK）活性顯著降低。在體外激酶測定中，Hesperadin（IC50 = 40 nM）阻斷了來自病原性錐蟲（Trypanosoma brucei）的TbAUK1（T. brucei Aurora kinase-1）對重組色質(zhì)組蛋白H3的磷酸化。Hesperadin（IC50 = 48 nM）顯著抑制了培養(yǎng)的傳染性血液形式（BF）細(xì)胞的生長，而以IC50 = 550 nM的濃度弱抑制了昆蟲循環(huán)階段（PF）細(xì)胞的生長。 |
| 存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | 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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| 關(guān)鍵字 | TbAUK1 | procyclic | Parasite | Inhibitor | inhibit | InfluenzaVirus | Influenza Virus | Hesperadin | forms | bloodstream | Autophagy | AuroraKinase | Aurora Kinase | Aurora B (human) | Aurora |
| 相關(guān)產(chǎn)品 | Guanidine hydrochloride | Naringin | Valproic Acid | Taurine | Urethane | Gefitinib | Doxycycline | Hydroxychloroquine | Stavudine | Paeonol | Sodium 4-phenylbutyrate | Kojic acid |
| 相關(guān)庫 | 抑制劑庫 | 經(jīng)典已知活性庫 | 抗癌化合物庫 | 已知活性化合物庫 | 細(xì)胞周期化合物庫 | 抗感染化合物庫 | 激酶抑制劑庫 | 抗衰老化合物庫 | 表觀遺傳庫 | 抗病毒庫 | 抗寄生蟲庫 | 膜蛋白靶向化合物庫 |