1. Signaling Pathways
  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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-12564
    Phthalazinone pyrazole
    Inhibitor ≥98.0%
    Phthalazinone pyrazole is a potent, selective, and orally active inhibitor of Aurora-A kinase with an IC50 of 0.031 μM. Phthalazinone pyrazole can arrests mitosis and subsequently inhibit tumor growth via apoptosis of proliferating cells. Phthalazinone pyrazole suppresses the epithelial-mesenchymal transition (EMT) during the differentiation of hepatocyte-like cells (HLCs) from human embryonic stem cells.
    Phthalazinone pyrazole
  • HY-N0110A
    Palmatine
    Inhibitor
    Palmatine 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 can also inhibit West Nile virus (WNV) NS2B-NS3 protease in an uncompetitive manner with an IC50 of 96 μM. Palmatine shows anti-cancer, anti-oxidation, anti-inflammatory, neuroprotection, antibacterial, anti-viral activities.
    Palmatine
  • HY-158038
    AurkA allosteric-IN-1
    Inhibitor
    AurkA allosteric-IN-1 (compound 6h) is an Aurora A (AurkA) inhibitor (IC50: 6.50 μM) that inhibits the catalytic activity and non-catalytic functions of Aurora A. Aurora A regulates the assembly of the bipolar mitotic spindle and the fidelity of chromosome segregation during mitosis and has non-catalytic functions. AurkA allosteric-IN-1 blocks the interaction of AurkA with the activator TPX2 by binding to the Y pocket of AurkA.
    AurkA allosteric-IN-1
  • HY-10971A
    Alisertib sodium
    Inhibitor
    Alisertib (MLN 8237) sodium 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 sodium induces apoptosis and autophagy through targeting the AKT/mTOR/AMPK/p38 pathway in leukemic cells. Antitumor activity.
    Alisertib sodium
  • 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-168540
    PROTAC MPS1 degrader 1
    Degrader
    PROTAC MPS1 degrader 1 (Compound 19) is a potent degrader of monopolar spindle 1 (Mps1, TTK), AURKA and AURKB, with DC50s of 17.7, 108.7 and 570.3 nM, respectively. PROTAC MPS1 degrader 1 can be used for the research of acute myeloid leukemia. (Pink: ligand for target protein (HY-168542); Black: linker (HY-W141926); Blue: ligand for E3 ligase (HY-10984).
    PROTAC MPS1 degrader 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-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-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-172144
    JB300
    Degrader
    JB300 is a highly selective Aurora A degrader based on PROTAC technology (DC50=30 nM). JB300 can be used for tumor research. JB300 consists of PROTAC target protein ligand MK-5108 (HY-13252) (pink part), E3 ligase ligand Thalidomide-O-COOH (HY-103597) (blue part) and PROTAC Linker Boc-NH-PEG2-C2-NH2 (HY-W008474) (black part), of which the conjugate of E3 ubiquitin ligase ligand + Linker is Thalidomide-O-COOH-NH2-C2-PEG2-NH-Boc (HY-172145).
    JB300
  • 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-161407
    AURKA-IN-1
    Inhibitor
    AURKA-IN-1 (compound 9) is an cell-active covalent AURKA inhibitor. AURKA-IN-1 is a lysine-reactive activity probe.
    AURKA-IN-1
  • HY-RS01266
    AURKA Human Pre-designed siRNA Set A
    Inhibitor

    AURKA Human Pre-designed siRNA Set A contains three designed siRNAs for AURKA gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

    AURKA Human Pre-designed siRNA Set A
  • HY-149694
    Aurora kinase inhibitor-12
    Inhibitor
    Aurora kinase inhibitor-12 (Compound 1a ) is the inhibitor of aurora kinase which is a key enzyme that is implicated in tumor growth.
    Aurora kinase inhibitor-12
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