1. Signaling Pathways
  2. Cell Cycle/DNA Damage
    Epigenetics
  3. Aurora Kinase

Aurora Kinase (极光激酶)

Aurora 激酶包括进化保守的丝氨酸/苏氨酸激酶家族(Aurora-A、Aurora-B 和 Aurora-C)。Aurora 激酶控制细胞周期进程中的多个事件,对有丝分裂和减数分裂双极纺锤体的组装和功能至关重要。

Aurora-A、Aurora-B 和 Aurora-C 共享高度保守的激酶结构域,但在有丝分裂期间具有完全不同的亚细胞定位和功能。Aurora-A 主要控制着丝粒成熟和双极纺锤体的组装,而 Aurora-B 和 Aurora-C 是 (前) 中期和细胞分裂期间染色体凝聚、附着于着丝粒和排列所必需的。在人类肿瘤中,所有 Aurora 激酶成员都发挥与其有丝分裂活动相关的致癌作用,并促进癌细胞存活和增殖。针对 Aurora 激酶的抑制剂已引起癌症研究的关注。

The Aurora kinases comprise a family of evolutionary conserved serine/threonine kinases (Aurora-A, Aurora-B, and Aurora-C). Aurora kinases control multiple events during cell cycle progression and are essential for mitotic and meiotic bipolar spindle assembly and function.

Aurora-A, Aurora-B, and Aurora-C share a highly conserved kinase domain but have quite different subcellular localizations and functions during mitosis. Aurora-A mostly controls centrosome maturation and bipolar spindle assembly, while Aurora-B and Aurora-C are required for condensation, attachment to kinetochores, and alignment of chromosomes during (pro-)metaphase and cytokinesis. In human tumors, all Aurora kinase members play oncogenic roles related to their mitotic activity and promote cancer cell survival and proliferation. Inhibitors targeting Aurora kinases have attracted attention in cancer research.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-123697
    VE-465 Inhibitor
    VE-465 是一种 Aurora 激酶抑制剂。VE-465 诱导癌细胞凋亡 (apoptosis)。VE-465 在多种肿瘤模型中具有抗癌作用。
    VE-465
  • HY-125090
    PHA-680626 Inhibitor
    PHA-680626 是 Aurora-AN-Myc 之间相互作用的有效抑制剂。PHA-680626 抑制 AURKA 和 Bcr-Abl 的激酶活性,并诱导 N-Myc 降解。PHA-680626 降低 CrkL 和组蛋白 H3 的磷酸化。PHA-680626 对 Imatinib (HY-15463) 耐药慢性粒细胞白血病细胞系和原代 CD34+ 细胞表现出抗增殖和促凋亡活性。
    PHA-680626
  • HY-121895
    BI 831266 Inhibitor
    BI 831266 是一种强效且选择性的 Aurora 激酶 B 抑制剂,具有抗肿瘤活性。
    BI 831266
  • HY-169735
    Aurora A inhibitor 4 Inhibitor
    Aurora A inhibitor 4 (compound C9) 是 Aurora A 的有效抑制剂,在 DU 145 细胞和 HT-29 细胞中的 GI50 分别为 4.26 和 7.08 μM。
    Aurora A inhibitor 4
  • HY-123279
    OM137 Inhibitor
    OM137 是一种 aurora 激酶 抑制剂,IC50 为 21.7 μM (Aurora A 激酶) 和 2.4 μM (Aurora B 激酶)。OM137 还抑制 Cdk1/cyclinB 和 Cdk5/p25,IC50 约为 20 μM。OM137 可降低染色体动粒处的纺锤体检查点信号蛋白 (Mad2 和 BubR1) 含量。
    OM137
  • HY-160447
    FAK/Aurora kinase-IN-1 Inhibitor
    FAK/Aurora Kinase-IN-1 是一种 FAK 和极光激酶 (aurora kinase) 抑制剂,IC50 值分别为 6.61 nM 和 0.91 nM。FAK/Aurora Kinase-IN-1 显示出抗癌作用 (WO2018019252A1; compound 11)。
    FAK/Aurora kinase-IN-1
  • HY-111506
    Aurora inhibitor 1 Inhibitor
    Aurora inhibitor 1 是一种有效的 Aurora 抑制剂,抑制 Aurora AAurora B 激酶的 IC50 分别 ≤4 nM 和 ≤13 nM。
    Aurora inhibitor 1
  • HY-U00304
    Aurora B inhibitor 1 Inhibitor
    Aurora B inhibitor 1 是一种 Aurora B (Aurora-1) 抑制剂,Ki 值 <0.010 uM。详细信息请参考专利文献 WO2007059299A1 中的化合物 1-3。
    Aurora B inhibitor 1
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