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

Aurora Kinase

Aurora Kinase

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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.

Aurora Kinase Isoform Specific Products:

Aurora Kinase Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-10127A
    Barasertib dihydrochloride
    		Inhibitor
    Barasertib (AZD1152 dihydrochloride), 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 dihydrochloride) induces growth arrest and apoptosis in cancer cells.
    Barasertib dihydrochloride
  • HY-10058
    AT9283 lactic acid
    		Inhibitor
    AT9283 lactic acid 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 lactic acid inhibits growth and survival of multiple solid tumors in vitro and in vivo.
    AT9283 lactic acid
  • HY-12054A
    Hesperadin hydrochloride
    		Inhibitor
    Hesperadin hydrochloride is an ATP competitive indolinone inhibitor of Aurora A and B. Hesperadin hydrochloride inhibits Aurora B with an IC50 of 250 nM.
    Hesperadin hydrochloride
  • HY-111506
    Aurora inhibitor 1
    		Inhibitor
    Aurora inhibitor 1 is a potent Aurora inhibitor with an IC50 of ≤ 4 nM and ≤13 nM for Aurora A and Aurora B kinase, respectively.
    Aurora inhibitor 1
  • HY-169505
    Aurora kinase inhibitor-13
    		Inhibitor
    Aurora kinase inhibitor-13 (Compound 2) is an inhibitor of Aurora kinase, with an IC50 value of 2.3 μM against Aurora kinase A.
    Aurora kinase inhibitor-13
  • HY-178343
    Aurora A-IN-5
    		Inhibitor
    Aurora A-IN-5 is a potent and highly selective Aurora A inhibitor (IC50 = 0.02 μM), showing 362-fold selectivity for over Aurora B. Aurora A-IN-5 shows its selectivity through unique C−H/π interactions, enhanced hydrophobic contacts, an open binding pocket, and tighter protein packing. Aurora A-IN-5 suppresses Aurora A autophosphorylation, thereby inhibiting cancer cell proliferation by inducing G2/M phase arrest, triggering apoptosis, and suppressing colony formation. Aurora A-IN-5 inhibits tumor growth in MDA-MB-231 xenograft mouse models. Aurora A-IN-5 can be used for breast, cervical, prostate, and lymphoma cancer research.
    Aurora A-IN-5
  • HY-149354
    Aurora kinase-IN-4
    		Inhibitor
    Aurora kinase-IN-4 (Compound 11c) is a covalent and ATP competitive aurora kinase A inhibitor (IC50: 1.7 nM). Aurora kinase-IN-4 inhibits cell proliferation in SJSA-1, MDA-MB-231, A54, HeLa cells with IC50s of 4.27, 1.54, 3.08, 6.99 μM. Aurora kinase-IN-4 can be used for research of triple negative breast cancer (TNBC).
    Aurora kinase-IN-4
  • HY-173499
    HLDA-212
    		Ligand
    HLDA-212 (Compound 43) is a bifunctional small molecule targeting HaloTag-tagged protein (Target Protein, TP) and Aurora kinase A/B (AURKA/B, Effector Protein, EP). HLDA-212 binds to TP and EP to form a stable ternary complex (TP:RIPTAC:EP), inhibiting the cell-survival function of EP and inducing apoptosis in TP-expressing cancer cells. HLDA-212 shows antiproliferative activity (GI50 of 0.011 μM) in 293_HFL cells. HLDA-212 is promising for research of cancers with high TP expression (such as prostate cancer and hematological malignancies).
    HLDA-212
  • HY-179374
    Aurora kinase/HDAC-IN-1
    		Inhibitor
    Aurora kinase/HDAC-IN-1 is an orally active dual Aurora kinase and HDAC inhibitor that inhibits Aurora A (IC50 = 116 nM), Aurora B (IC50 = 225 nM), HDAC1 (IC50 = 164 nM), and HDAC2 (IC50 = 346 nM).Aurora kinase/HDAC-IN-1 promotes histone H3 acetylation, inhibits Aurora A phosphorylation and downstream signaling, and induces apoptosis via G2/M cell-cycle arrest. Aurora kinase/HDAC-IN-1 exhibits potent antiproliferative activity in colorectal cancer cells, with an IC50 value of 30.2 nM in HCT-116 cells.Aurora kinase/HDAC-IN-1 significantly suppresses tumor growth in an HCT-116 colorectal cancer xenograft mouse model.
    Aurora kinase/HDAC-IN-1
  • HY-181082
    Aurora kinase-IN-10
    		Inhibitor
    Aurora kinase-IN-10 is an Aurora kinase inhibitor. Aurora kinase-IN-10 exhibits IC50 values of 5.94 nM and 86.06 nM against Aurora A and Aurora B, respectively. Aurora kinase-IN-10 has anti-tumor activity and can be used in the research of tumors such as triple-negative breast cancer.
    Aurora kinase-IN-10
  • HY-183102
    ATC12
    		Inhibitor
    ATC12 is a Aurora-A kinase inhibitor. ATC12 binds to Aurora-A and competes with TPX2 for binding to disrupt the Aurora-A/TPX2 interaction. ATC12 inhibits cancer cell proliferation, induces apoptosis and cellular senescence. ATC12 can be used in the research of breast cancer.
    ATC12
  • HY-186210
    TACC3-IN-5
    TACC3-IN-5 (Compound 35) 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-5 inhibits the proliferation of triple-negative breast cancer cells. TACC3-IN-5 is applicable for triple-negative breast cancer research.
    TACC3-IN-5
  • HY-179641
    SK5527
    		Degrader
    SK5527 is a selective AURKA PROTAC degrader degrading AURKA with DC50 = 2 nM. SK5527 bind to NanoLuc-AURKA with an IC50 of 20 nM. SK5527 effectively reduces MYCN levels in MYCN-amplified neuroblastoma cells and limited by MDR1-mediated efflux. SK5527 efficiently reduced AURKA levels in vivo. SK5527 can be used for neuroblasto2ma research.
    SK5527
  • HY-179375
    LCI133
    		Inhibitor
    LCI133 is afirst-in-class,nanomolar-potent, selective multikinase inhibitor targeting CDK4/6/9 and AURKA/B (IC50 = 4.7/10.2/4.1 nM and 2.8/10.6 nM). LCI133 induces S/G2 cell-cycle arrest and robust apoptosis in MYCN-amplified neuroblastoma BE(2)-C cells. LCI133 demonstrates significant antitumor efficacy in a BE(2)-C neuroblastoma xenograft model.
    LCI133
  • HY-137344
    dAURK-4
    		Inhibitor
    dAURK-4, an Alisertib (HY-10971) derivative, is a potent and selective AURKA (Aurora A) degrader. dAURK-4 has anticancer effects.
    dAURK-4
  • HY-155464
    VEGFR-2/AURKA-IN-1
    		Chemical
    VEGFR-2/AURKA-IN-1 (compound 5e) is a thiazolidin-4-one derivative with antiglioma activity (IC50: 6.43 μM, LN229). VEGFR-2/AURKA-IN-1 has affinity for AURKA and VEGFR-2 and is a potential ligand. VEGFR-2/AURKA-IN-1 causes DNA strand breaks and exhibits cytotoxic and anticancer potential.
    VEGFR-2/AURKA-IN-1
  • HY-179574
    AURKA-IN-4
    		Inhibitor
    AURKA-IN-4 (compound 13), a capsaicin-derived prohibitin ligand, is an AURKA inhibitor. AURKA-IN-4 acts as a molecular glue within the AURKA/PHB2/LC3 complex. AURKA-IN-4 is specific to the mitochondrial pool of AURKA, and inhibits AURKA-dependent mitophagy. AURKA-IN-4 can be used for cancer research.
    AURKA-IN-4
  • HY-168718
    FAK-IN-22
    		Inhibitor
    FAK-IN-22 (Compound 26) is an inhibitor of FAK, JAK3, and Aurora B, with IC50 values of 50.94 nM, 9.99 nM, and 0.49 nM, respectively, effectively inhibiting tumor occurrence and metastasis in pancreatic ductal adenocarcinoma (PDAC). FAK-IN-22 effectively inhibits the proliferation of PANC-1 cells, with an IC50 value of 0.15 μM. FAK-IN-22 induces apoptosis and G2/M phase arrest in PANC-1 cells by inhibiting the FAK/PI3K/Akt signaling pathway.
    FAK-IN-22
  • HY-158618
    Aurora kinase inhibitor-14
    		Inhibitor
    Aurora kinase inhibitor-14 (Compound 79) is an orally active and highly selective inhibitor of Aurora kinases with IC50 values of 0.5 nM and 1.2 nM for Aurora A and Aurora B, respectively. Aurora kinase inhibitor-14 binds to the ATP-binding site of Aurora kinases to block chromosome segregation during mitosis and induce apoptosis in tumor cells. Aurora kinase inhibitor-14 is promising for research of various solid tumors and hematological malignancies, such as non-small cell lung cancer, breast cancer, and acute myeloid leukemia.
    Aurora kinase inhibitor-14
  • HY-19565
    KW-2450 tosylate
    		Inhibitor
    KW-2450 tosylate is an orally active Aurora A and B kinases, IGF-1R, and IR tyrosine kinases inhibitor. KW-2450 tosylate induces Apoptosis. KW-2450 tosylate also exhibits anticancer activity against triple-negative breast cancer.
    KW-2450 tosylate
Cat. No. Product Name / Synonyms Application Reactivity
Aurora Kinase Isoform Comparison

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