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Home >> Signaling Pathways >> Chromatin/Epigenetics >> Aurora Kinase

Aurora Kinase(极光激酶)

Aurora kinases are a family of serine-threonine kinases of three highly homologous members, including aurora A kinase, aurora B kinase and aurora C kinase, which are responsible for chromosome assembly and segregation during mitosis. Aurora kinases are characterized by two domains: a regulatory domain in the NH2 terminus and a catalytic domain in the COOH terminus, in which an A-Box and a D-Box found correspondingly in each domain are responsible for protein degradation. Aurora A kinase plays an important role in centrosome function and duplication, mitotic entry and bipolar spindle assembly; while Aurora B kinase is the catalytic component of the chromosomal passenger complex regulating the accurate segregation of the chromatids at mitosis, histone modification and cytokinesis. Aurora C kinase is less studied and expressed restrictedly in the testes.

Products for  Aurora Kinase

  1. Cat.No. 产品名称 Information
  2. GC35216 AAPK-25 AAPK-25 是一种有效选择性的 Aurora/PLK 激酶双重抑制剂，具有抗肿瘤活性。AAPK-25 可引起有丝分裂延迟并阻滞前中期细胞，通过生物标志物组蛋白 H3Ser10 磷酸化反应，随后细胞凋亡激增。AAPK-25 靶向 Aurora-A, -B, -C 的 Kd 值为 23 nM-289 nM，靶向 PLK-1, -2, -3 的 Kd 值为 55-456 nM。
  3. GC62433 AKI603 AKI-603 is an inhibitor of Aurora kinase A (AurA), which is developed to overcome resistance mediated by BCR-ABL-T315I mutation.
  4. GC13198 AMG-900 A selective pan-Aurora kinase inhibitor
  5. GC17284 Anacardic acid

    漆树酸; Hydroginkgolic acid; Ginkgolic Acid C15

    A histone acetyltransferase inhibitor
  6. GC10638 AT9283 A broad spectrum kinase inhibitor
  7. GC72964 Aurkin A Aurkin A是极光A激酶（Aurora A Kinase，也称Aurka）与TPX2相互作用的变抗抑制剂，通过靶向TPX2结合位点，Kd为3.77 μM。
  8. GC13332 Aurora A Inhibitor I A potent and selective inhibitor of Aurora A kinase
  9. GC33379 Aurora B inhibitor 1 AuroraBinhibitor1是一种AuroraB(Aurora-1)抑制剂，Ki值<0.010uM。详细信息请参考专利文献WO2007059299A1中的化合物1-3。
  10. GC40667 Aurora Kinase Inhibitor II

    4-(4-Benzamidoanilino)-6,7-dimethoxyquinazoline

     Blocks Aurora A kinase activity
  11. GC15711 Aurora Kinase Inhibitor III A potent inhibitor of Aurora A kinase
  12. GC67899 Aurora kinase inhibitor-8 Aurora kinase inhibitor-8 是一种高选择性 Aurora 激酶的抑制剂。
  13. GC73375 Aurora Kinases-IN-3 Aurora Kinases-IN-3（化合物15a）是一种口服活性AURKB抑制剂，通过破坏AURKB的有丝分裂定位来引发AURKB抑制活性。
  14. GC48971 AZD 1152 (hydrochloride)

    5-[[7-[3-[乙基[2-(磷酰氧基)乙基]氨基]丙氧基]-4-喹唑啉基]氨基]-N-(3-氟苯基)-1H-吡唑-3-乙酰胺二盐酸盐

     A prodrug for a potent Aurora B inhibitor
  15. GC14709 AZD1152

    5-[[7-[3-[乙基[2-(磷酰氧基)乙基]氨基]丙氧基]-4-喹唑啉基]氨基]-N-(3-氟苯基)-1H-吡唑-3-乙酰胺,AZD-1152;AZD 1152

     AZD1152 (AZD1152) 是 AZD1152-hQPA 的前药，是一种高选择性的 Aurora B 抑制剂，在无细胞试验中 IC50 为 0.37 nM。 AZD1152 (AZD1152) 在癌细胞中诱导生长停滞和凋亡。
  16. GC14955 Barasertib (AZD1152-HQPA)

    5-[[7-[3-[乙基(2-羟基乙基)氨基]丙氧基]-4-喹唑啉]氨基]-N-(3-氟苯基)-1H-吡唑-3-乙酰胺,AZD1152-HQPA,AZD-1152HQPA, AZD1152 HPQA,INH 34

     A selective Aurora kinase B inhibitor
  17. GC17828 BI-847325 A selective dual MEK/Aurora kinase inhibitor
  18. GC42933 Binucleine 2 An inhibitor of Drosophila Aurora B kinase
  19. GC11310 CCT129202

    2-[4-[6-氯-2-(4-二甲基氨基苯基)-3H-咪唑并[4,5-B]吡啶-7-基]哌嗪-1-基]-N-(噻唑-2-基)乙酰胺,CCT-129202, CCT 129202

     An Aurora kinase inhibitor
  20. GC14566 CCT137690

    甲磺酸阿贝西尼

     An inhibitor of Aurora kinases and FLT3
  21. GC19092 CCT241736 A dual inhibitor of Aurora kinases and FLT3
  22. GC48982 CD532 An inhibitor of Aurora A kinase activity and the Aurora A-N-Myc protein-protein interaction
  23. GC62189 CD532 hydrochloride An inhibitor of Aurora A kinase activity and the Aurora A-N-Myc protein-protein interaction
  24. GC35651 Cenisertib

    AS-703569; R-763

     Cenisertib (AS-703569) 是一种多激酶抑制剂，可抑制 Aurora-kinase-A/B，ABL1，AKT，STAT5, FLT3 的活性。 Cenisertib 通过抑制肿瘤肥大细胞 (MC) 中几种不同分子靶标的活性抑制其生长。 Cenisertib 抑制异种移植模型中胰腺癌，乳腺癌，结肠癌，卵巢癌和肺癌以及白血病的肿瘤生长。
  25. GC62145 Chiauranib

    CS2164

     Chiauranib (CS2164) selectively inhibits multiple kinase targets aurora B kinase (AURKB), colony-stimulating factor 1 receptor (CSF1R), and vascular endothelial growth factor receptor (VEGFR)/platelet-derived growth factor receptor (PDGFR)/c-Kit , thereby inhibiting the rapid proliferation of tumor cells, enhancing the antitumor immunity, and inhibiting tumor angiogenesis, to achieve the anti-tumor efficacy.
  26. GC15106 CYC116 A potent Aurora kinase inhibitor
  27. GC15217 Danusertib (PHA-739358)

    达鲁舍替,5-Amido-pyrrolopyrazole 9d

     A pan-Aurora kinase and Abl inhibitor
  28. GC68147 dAURK-4 hydrochloride dAURK-4 hydrochloride 是 Alisertib 的一种衍生物，是一种有效的选择性 AURKA (Aurora A) 降解剂。dAURK-4 hydrochloride 具有抗癌作用。
  29. GC74000 DBPR728 DBPR728是6K465的酰基前药，携带较少的氢键供体。
  30. GC73753 EGFR/AURKB-IN-1 EGFR/AURKB-IN-1（化合物7）是双靶向EGFR/AURKB抑制剂，抑制L858R EGFR和AURKB的磷酸化，ic50值分别为0.07和1.1。
  31. GC16519 ENMD-2076

    6-(4-甲基-1-哌嗪基)-N-(5-甲基-1H-吡唑-3-基)-2-[(1E)-2-苯乙烯基]-4-嘧啶胺

     A multi-kinase inhibitor
  32. GC12145 ENMD-2076 L-(+)-Tartaric acid ENMD-2076 L-(+)-Tartaric acid 是一种多靶点激酶抑制剂，对 Aurora A、Flt3、KDR/VEGFR2、Flt4/VEGFR3、FGFR1 的 IC50 为 1.86、14、58.2、15.9、92.7、70.8、56.4 nM , FGFR2, Src, PDGFRα, 分别。
  33. GC69068 ENMD-2076 Tartrate ENMD-2076 Tartrate 是多靶点激酶抑制剂，抑制 Aurora A，Flt3，KDR/VEGFR2，Flt4/VEGFR3，FGFR1，FGFR2，Src，PDGFRα 的IC50 值分别为1.86，14，58.2，15.9，92.7，70.8，20.2 and 56.4 nM。
  34. GC10008 GSK1070916

    GSK-1070916A

     A potent inhibitor of Aurora B and C kinases
  35. GC17196 Hesperadin A multi-kinase inhibitor
  36. GC50050 Hesperadin hydrochloride A multi-kinase inhibitor
  37. GC34159 Ilorasertib (ABT-348)

    ABT-348

     A multi-kinase inhibitor
  38. GC38519 Ilorasertib hydrochloride

    ABT-348 hydrochloride

     A multi-kinase inhibitor
  39. GC73744 JAB-2485 JAB-2485是一种有效的选择性极光激酶a （AURKA）抑制剂，IC50为0.33 nM。
  40. GC12612 JNJ-7706621

    JNJ7706621, JNJ 7706621

     A dual inhibitor of CDKs and Aurora kinases
  41. GC14592 KW 2449

    [4-[2-(1H-吲唑-3-基)乙烯基]苯基]-1-哌嗪基甲酮

     A multi-kinase inhibitor
  42. GC33057 LY3295668 (AK-01)

    AK-01

     LY3295668 (AK-01) is a potent, orally active and specific inhibitor of Aurora A kinase with Ki of 0.8 nM and 1038 nM for AURKA and AURKB, respectively.
  43. GC17162 MK-5108 (VX-689)

    VX-689

     A potent inhibitor of Aurora kinases
  44. GC10442 MK-8745 An Aurora A kinase inhibitor
  45. GC12208 MLN8054

    4-[[9-氯-7-(2,6-二氟苯基)-5H-嘧啶并[5,4-D][2]苯并氮杂卓-2-基]氨基]苯甲酸

     An inhibitor of Aurora A kinase
  46. GC12690 MLN8237 (Alisertib)

    阿立塞替,MLN 8237

     Alisertib (MLN8237) 作为一种在研、可口服的选择性极光 A 激酶抑制剂，通常用于治疗实体瘤和血液系统恶性肿瘤。
  47. GC34692 NU6140 A Cdk2 inhibitor
  48. GC18074 PF-03814735

    N-[2-[(1S,4R)-6-[[4-(环丁基氨基)-5-(三氟甲基)-2-嘧啶基]氨基]-1,2,3,4-四氢萘-1,4-亚氨-9-基]-2-氧代乙基]乙酰胺

     PF-03814735 是一种有效的、具有口服生物利用度的 Aurora1 和 Aurora2 激酶的可逆抑制剂，IC50 值分别为 0.8nM 和 5nM 。
  49. GC10479 PHA-680632

    Pha 680632

     An Aurora kinase inhibitor
  50. GC13668 Phthalazinone pyrazole Potent, selective inhibitor of Aurora kinase A
  51. GC14651 Reversine

    逆转素

     Reversine是一种靶向Aurora A激酶、Aurora B激酶和MPS1（Monopolar Spindle 1）激酶的非特异性、具有口服活性的小分子抑制剂。Reversine常用于细胞分化和多种癌症的研究。

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