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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. GC74000 DBPR728 DBPR728是6K465的酰基前药，携带较少的氢键供体。
  3. 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。
  4. 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。
  5. 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。
  6. 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。
  7. GC70030 Tinengotinib Tinengotinib 是一种或多种蛋白激酶的调节剂，例如 Aurora 激酶和 VEGFR 激酶。Tinengotinib 具有研究这些激酶异常介导的疾病的潜力，尤其是癌症相关疾病 (摘自专利 WO2018108079A1)。
  8. 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。
  9. GC25940 SNS-314 SNS-314 is a potent and selective inhibitor of Aurora A, Aurora B and Aurora C with IC50 of 9 nM, 31 nM, and 3 nM, respectively. It is less potent to Trk A/B, Flt4, Fms, Axl, c-Raf and DDR2. Phase 1.
  10. 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。
  11. GC67899 Aurora kinase inhibitor-8 Aurora kinase inhibitor-8 是一种高选择性 Aurora 激酶的抑制剂。
  12. GC48982 CD532 An inhibitor of Aurora A kinase activity and the Aurora A-N-Myc protein-protein interaction
  13. 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
  14. GC62482 TAS-119 TAS-119 是一种有效的，选择性的，具有口服活性的 Aurora A 抑制剂，IC50 为 1.0 nM。TAS-119 对 Aurora A 的选择性高于其他蛋白激酶，包括 Aurora B (IC50 为 95 nM)。TAS-119 具有有效的抗肿瘤活性。
  15. GC62433 AKI603 AKI-603 is an inhibitor of Aurora kinase A (AurA), which is developed to overcome resistance mediated by BCR-ABL-T315I mutation.
  16. GC62189 CD532 hydrochloride An inhibitor of Aurora A kinase activity and the Aurora A-N-Myc protein-protein interaction
  17. 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.
  18. GC50050 Hesperadin hydrochloride A multi-kinase inhibitor
  19. GC38519 Ilorasertib hydrochloride

    ABT-348 hydrochloride

     A multi-kinase inhibitor
  20. GC37606 SCH-1473759 hydrochloride SCH-1473759 hydrochloride是多靶点的的极光激酶 (aurora) 抑制剂，对极光激酶A和B的IC50 值分别为4 和13 nM。
  21. 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。
  22. 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。
  23. GC42933 Binucleine 2 An inhibitor of Drosophila Aurora B kinase
  24. GC40667 Aurora Kinase Inhibitor II

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

     Blocks Aurora A kinase activity
  25. GC34692 NU6140 A Cdk2 inhibitor
  26. GC34159 Ilorasertib (ABT-348)

    ABT-348

     A multi-kinase inhibitor
  27. 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。
  28. 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.
  29. GC19092 CCT241736 A dual inhibitor of Aurora kinases and FLT3
  30. GC15711 Aurora Kinase Inhibitor III A potent inhibitor of Aurora A kinase
  31. GC13668 Phthalazinone pyrazole Potent, selective inhibitor of Aurora kinase A
  32. GC17828 BI-847325 A selective dual MEK/Aurora kinase inhibitor
  33. GC10442 MK-8745 An Aurora A kinase inhibitor
  34. GC17455 TAK-632 A selective pan-Raf inhibitor
  35. GC16378 TC-A 2317 hydrochloride TC-A 2317 hydrochloride 是一种具有口服活性的 Aurora A 激酶抑制剂 (Ki=1.2 nM)。 TC-A 2317 hydrochloride 对 Aurora B 激酶 (Ki=101 nM) 和其他 60 种激酶具有出色的选择性、良好的细胞渗透性和良好的 PK 曲线。抗肿瘤活性。
  36. GC17284 Anacardic acid

    漆树酸; Hydroginkgolic acid; Ginkgolic Acid C15

    A histone acetyltransferase inhibitor
  37. GC13102 XL228

    N4-(5-环丙基-1H-吡唑-3-基)-N2-[[3-异丙基-5-异恶唑基]甲基]-6-(4-甲基-1-哌嗪基)-2,4-嘧啶二胺,XL-228;XL 228

     A tyrosine kinase inhibitor
  38. GC16614 SCH-1473759

    SCH1473759;SCH 1473759

     SCH-1473759 是一种极光抑制剂，对极光 A 和 B 的 IC50 分别为 4 和 13 nM。
  39. 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。
  40. 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。
  41. 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 。
  42. GC10008 GSK1070916

    GSK-1070916A

     A potent inhibitor of Aurora B and C kinases
  43. GC13332 Aurora A Inhibitor I A potent and selective inhibitor of Aurora A kinase
  44. GC15106 CYC116 A potent Aurora kinase inhibitor
  45. GC11085 TAK-901

    5-[3-(乙基磺酰基)苯基]-3,8-二甲基-N-(1-甲基-4-哌啶基)-9H-吡啶并[2,3-B]吲哚-7-甲酰胺

     A non-selective inhibitor of Aurora kinases
  46. 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
  47. GC10479 PHA-680632

    Pha 680632

     An Aurora kinase inhibitor
  48. GC13837 SNS-314 Mesylate

    N-(3-氯苯基)-N'-[5-[2-(噻吩并3,2-D]嘧啶-4-基氨基)乙基]-2-噻唑基]脲甲磺酸盐(1:1)

     A pan-Aurora kinase inhibitor
  49. GC17162 MK-5108 (VX-689)

    VX-689

     A potent inhibitor of Aurora kinases
  50. GC13198 AMG-900 A selective pan-Aurora kinase inhibitor
  51. GC17196 Hesperadin A multi-kinase inhibitor

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