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Aurora Kinase


Aurora kinases are serine/threonine kinases that are essential for cell proliferation. The enzyme helps the dividing cell dispense its genetic materials to its daughter cells. More specifically, Aurora kinases play a crucial role in cellular division by controlling chromatid segregation. Defects in this segregation can cause genetic instability, a condition which is highly associated with tumorigenesis.
There are three classes of aurora kinases:Aurora A (aka, Aurora 2) functions during prophase of mitosis and is required for correct function of the centrosomes (the microtubule organising centres in eukaryotic cells);Aurora B (aka, Aurora 1) functions in the attachment of the mitotic spindle to the centromere;Aurora C (AURKC) works in germ-line cells and little is known about its function.

  • BI-847325 EY2849

    BI-847325是一种口服具有生物活性的选择性的双重MEK/Aurora kinase抑制剂,对人类MEK2和AK-C的IC50值分别为4和15 nM。

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  • Barasertib EY1808

    AZD1152-HQPA是AZD-1152的活性代谢物,AZD1152-HQPA (Barasertib)是Aurora B 高选择性抑制剂,IC50为0.37 nM,比对Aurora A的抑制性高100倍。

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  • Alisertib EY1556

    Alisertib (MLN8237)是一种选择性的Aurora A抑制剂,IC50为1.2 nM,作用于Aurora A比作用于Aurora B选择性强200倍以上。

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  • ZM 447439 EY1434

    ZM 447439是ATP竞争性Aurora A和B选择性抑制剂,IC50分别为110 nM和130 nM。

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  • VX-680 EY1314

    Tozasertib (MK-0457; VX-680) 是Aurora抑制剂,对于Aurora-A,-B和-C的Ki分别为 0.6,18和4.6 nM。

    More
  • BI-847325 EY2849

    BI-847325是一种口服具有生物活性的选择性的双重MEK/Aurora kinase抑制剂,对人类MEK2和AK-C的IC50值分别为4和15 nM。

    More
  • Barasertib EY1808

    AZD1152-HQPA是AZD-1152的活性代谢物,AZD1152-HQPA (Barasertib)是Aurora B 高选择性抑制剂,IC50为0.37 nM,比对Aurora A的抑制性高100倍。

    More
  • Alisertib EY1556

    Alisertib (MLN8237)是一种选择性的Aurora A抑制剂,IC50为1.2 nM,作用于Aurora A比作用于Aurora B选择性强200倍以上。

    More
  • ZM 447439 EY1434

    ZM 447439是ATP竞争性Aurora A和B选择性抑制剂,IC50分别为110 nM和130 nM。

    More
  • VX-680 EY1314

    Tozasertib (MK-0457; VX-680) 是Aurora抑制剂,对于Aurora-A,-B和-C的Ki分别为 0.6,18和4.6 nM。

    More
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