1. シグナル伝達
  2. Cell Cycle/DNA Damage
    Epigenetics
  3. Aurora Kinase

Aurora Kinase

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.

製品番号 製品名 製品効果 純度 構造式
  • HY-10971
    Alisertib Inhibitor 99.84%
    Alisertib (MLN 8237) is an orally active and selective Aurora A kinase inhibitor (IC50=1.2 nM), which binds to Aurora A kinase resulting in mitotic spindle abnormalities, mitotic accumulation. Alisertib (MLN 8237) induces apoptosis and autophagy through targeting the AKT/mTOR/AMPK/p38 pathway in leukemic cells. Antitumor activity.
    Alisertib
  • HY-10127
    Barasertib Inhibitor 99.50%
    Barasertib (AZD1152), a pro-drug of Barasertib-hQPA, is a highly selective Aurora B inhibitor with an IC50 of 0.37 nM in a cell-free assay. Barasertib (AZD1152) induces growth arrest and apoptosis in cancer cells.
    Barasertib
  • HY-10126
    Barasertib-HQPA

    Barasertib-HQPA

    Inhibitor 98.90%
    Barasertib-HQPA (AZD2811) is a highly selective Aurora B inhibitor with an IC50 of 0.37 nM in a cell-free assay. Barasertib-HQPA (AZD2811) induces growth arrest and apoptosis in cancer cells.
    Barasertib-HQPA
  • HY-14711
    Reversine

    Reversine

    Inhibitor 99.22%
    Reversine is a novel class of ATP-competitive Aurora kinase inhibitor with IC50s of 400, 500 and 400 nM for Aurora A, Aurora B and Aurora C, respectively.
    Reversine
  • HY-10161
    Tozasertib

    Tozasertib

    Inhibitor 99.92%
    Tozasertib (VX 680; MK-0457) is an inhibitor of Aurora A/B/C kinases with Kis of 0.6, 18, 4.6 nM, respectively.
    Tozasertib
  • HY-181311
    CCT400028 Degrader 98.03%
    CCT400028 is a PROTACs-class degrader that targets the Aurora A (AURKA) kinase. CCT400028 induces ubiquitination and proteasomal degradation of target proteins by recruiting the cereblon (CRBN) E3 ubiquitin ligase. The KD values of CCT400028 against the three subtypes of human AURKA are 71 nM, 2100 nM and >10000 nM, respectively, and its IC50 against human CRBN is 6300 nM. CCT400028 is applicable to relevant research on leukemia, neuroblastoma and glioma.
    CCT400028
  • HY-180132
    PROTAC AURKA degrader 2 Degrader 98.36%
    PROTAC AURKA degrader 2 (compound D) is a potent and selective PROTAC AURKA degrader with an IC50 of 3.58 nM. PROTAC AURKA degrader 2 exhibits 21.6-fold selectivity for AURKA over AURKB (IC50 = 77.2 nM). PROTAC AURKA degrader 2 specifically depletes AURKA on the mitotic spindle.
    PROTAC AURKA degrader 2
  • HY-186208
    TACC3-IN-3
    TACC3-IN-3 is a TACC3 inhibitor. TACC3 is a scaffold protein that is highly expressed in various tumors and regulates microtubule/centrosome stability via phosphorylation by Aurora A. TACC3-IN-3 inhibits the proliferation of triple-negative breast cancer cells. TACC3-IN-3 is applicable to triple-negative breast cancer research.\n
    TACC3-IN-3
  • HY-B0712B
    Ceftriaxone sodium salt Inhibitor 99.90%
    Ceftriaxone sodium salt (Ro 13-9904) is a broad spectrum β-lactam third-generation cephalosporin antibiotic, which has good antibacterial activity against a variety of gram-negative and positive bacteria. Ceftriaxone sodium salt is a covalent inhibitor of GSK3β with IC50 value of 0.78 μM. Ceftriaxone sodium salt is an inhibitor of Aurora B. Ceftriaxone sodium salt has anti-inflammatory, antitumor and antioxidant activities. Ceftriaxone sodium salt can be used in the study of bacterial infections and meningitis.
    Ceftriaxone sodium salt
  • HY-N0110
    Palmatine chloride

    Palmatine (chloride)

    Inhibitor 99.87%
    Palmatine chloride is an orally active and irreversible indoleamine 2,3-dioxygenase 1 (IDO-1) inhibitor with IC50s of 3 μM and 157μM against HEK 293-hIDO-1 and rhIDO-1, respectively. Palmatine chloride can also inhibit West Nile virus (WNV) NS2B-NS3 protease in an uncompetitive manner with an IC50 of 96 μM. Palmatine chloride shows anti-cancer, anti-oxidation, anti-inflammatory, neuroprotection, antibacterial, anti-viral activities.
    Palmatine chloride
  • HY-B0712
    Ceftriaxone Inhibitor 99.87%
    Ceftriaxone (Ro 13-9904 free acid) is a broad spectrum β-lactam third-generation cephalosporin antibiotic, which has good antibacterial activity against a variety of gram-negative and positive bacteria. Ceftriaxone is a covalent inhibitor of GSK3β with IC50 value of 0.78 μM. Ceftriaxone is an inhibitor of Aurora B. Ceftriaxone has anti-inflammatory, antitumor and antioxidant activities. Ceftriaxone can be used in the study of bacterial infections and meningitis.
    Ceftriaxone
  • HY-10329
    JNJ-7706621

    JNJ-7706621

    Inhibitor 99.39%
    JNJ-7706621 is a potent aurora kinase inhibitor, and also inhibits CDK1 and CDK2, with IC50s of 9 nM, 3 nM, 11 nM, and 15 nM for CDK1, CDK2, aurora-A and aurora-B, respectively.
    JNJ-7706621
  • HY-12054
    Hesperadin

    Hesperadin

    Inhibitor 98.89%
    Hesperadin is an ATP competitive indolinone inhibitor of Aurora A and B. Hesperadin inhibits Aurora B with an IC50 of 250 nM. Hesperadin inhibits the growth of Trypanosoma brucei by blocking nuclear division and cytokinesis. Hesperadin also is a broad-spectrum influenza antiviral.
    Hesperadin
  • HY-10128
    ZM-447439

    ZM-447439

    Inhibitor 99.19%
    ZM-447439 is an aurora kinase inhibitor with IC50s of 110 and 130 nM for aurora A and B, respectively.
    ZM-447439
  • HY-10339
    KW-2449 Inhibitor 99.91%
    KW-2449 is a multi-targeted kinase inhibitor of FLT3, ABL, ABLT315I and Aurora kinase with IC50s of 6.6, 14, 4 and 48 nM, respectively.
    KW-2449
  • HY-10179
    Danusertib Inhibitor 99.08%
    Danusertib is a pyrrolo-pyrazole and aurora kinase inhibitor with IC50 of 13, 79, and 61 nM for Aurora A, B, and C, respectively.
    Danusertib
  • HY-50514
    AT9283

    AT9283

    Inhibitor 99.67%
    AT9283 is a multi-targeted kinase inhibitor with potent activity against Aurora A/B, JAK2/3, Abl (T315I) and Flt3 (IC50s ranging from 1 to 30 nM). AT9283 inhibits growth and survival of multiple solid tumors in vitro and in vivo.
    AT9283
  • HY-114258
    LY3295668 Inhibitor 99.76%
    LY3295668 (AK-01) is a highly specific and orally active inhibitor of Aurora-A kinase with a Ki values for AurA and AurB of 0.8 nM and 1038 nM respectively. LY3295668 can effectively inhibit the autophosphorylation of AurA, induce mitotic arrest and apoptosis. LY3295668 avoids the formation of polyploids related to AurB inhibition. LY3295668 can be used for the study of small cell lung cancer.
    LY3295668
  • HY-13253
    AMG 900 Inhibitor 98.82%
    AMG 900 is a potent and highly selective pan-Aurora kinases inhibitor with IC50 of 5 nM, 4 nM and 1 nM for Aurora A, B and C, respectively.
    AMG 900
  • HY-13252
    MK-5108 Inhibitor 99.60%
    MK-5108 is a highly potent and specific inhibitor of Aurora A kinase with an IC50 value of 0.064 nM.
    MK-5108
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