Aurora A
Aurora A kinase (AURKA) is a conserved serine/threonine kinase that primarily regulates centrosome maturation, centrosome separation, and bipolar spindle assembly during mitosis, thereby supporting accurate chromosome segregation and cell-cycle progression[1][2]. Mechanistically, AURKA functions within mitotic spindle regulatory networks and is activated through interactions with spindle-associated cofactors such as TPX2, which promotes spatial control of kinase activity during mitosis[3][4]. Through its role in microtubule organization and spindle formation, AURKA contributes to the maintenance of genomic stability, whereas dysregulated AURKA activity is associated with abnormal mitotic progression and chromosomal instability in cancer models[1][5]. In disease-relevant experimental systems, aberrant Aurora kinase signaling has been linked to tumor development and progression, supporting the use of AURKA as a molecular target in studies of mitotic control and oncogenic transformation[5][6]. Compared with related isoforms, Aurora B predominantly regulates chromosome-microtubule attachment, spindle checkpoint signaling, chromosome alignment, and cytokinesis as a core component of the chromosomal passenger complex, whereas AURKA mainly functions at centrosomes and spindle poles during early mitosis[1][2][3]. This spatial and functional distinction provides an important framework for isoform-selective experimental design and interpretation of mitotic phenotypes[1][3]. For research applications, Aurora kinase inhibitors are widely used to investigate mitotic signaling pathways and chromosome segregation mechanisms, and selective targeting strategies continue to be explored in anticancer research models[6].
References:
- [1]. Willems E, et al. The functional diversity of Aurora kinases: a comprehensive review. Cell Div. 2018 Sep 19;13:7. [Content Brief]
- [2]. Carmena M, et al. The cellular geography of aurora kinases. Nat Rev Mol Cell Biol. 2003;4(11):842-854.
- [3]. Carmena M, et al. Making the Auroras glow: regulation of Aurora A and B kinase function by interacting proteins. Curr Opin Cell Biol. 2009 Dec;21(6):796-805. [Content Brief]
- [4]. Wikipedia.
- [5]. Pérez de Castro I, et al. Editorial: Aurora Kinases: Classical Mitotic Roles, Non-Canonical Functions and Translational Views. Front Oncol. 2017;7:48.
- [6]. Kitzen JJ, et al. Aurora kinase inhibitors. Crit Rev Oncol Hematol. 2010 Feb;73(2):99-110. [Content Brief]
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Aurora A Related Products (114)
Related Products (114)
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Antibodies (2)
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LS-Q2
0 ImagesCat. No.: HY-182986LS-Q2 is a highly selective CDK4/9 inhibitor with IC50 values of 1.4 nM and 6.2 nM. LS-Q2 inhibits cancer cells proliferation, induces G2/M phase arrest, apoptosis and reduces pSer2 RNA polymerase II expression. LS-Q2 interacts synergistically with BET and Bcl-2 inhibitors to drive antitumor activity. LS-Q2 can be used for the research of cancer, such as malignant solid tumors.
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AURKA-IN-3
0 ImagesCat. No.: HY-175982AURKA-IN-3 (Compound AL8) is an irreversible covalent Aurora kinase A (AURKA) inhibitor with an IC50 value of 23.0 nM. AURKA-IN-3 inhibits the activation of cAMP signaling pathway and phospholipase C (PLC) signaling pathway mediated by AURKA, and reduces the autophosphorylation level of AURKA. AURKA-IN-3 is promising for research of malignant tumors associated with high AURKA expression (e.g., leukemia, lymphoma).
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LY3295668 erbumine
0 ImagesSynonyms: AK-01 erbumineLY3295668 (AK-01) erbumine 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 erbumine can effectively inhibit the autophosphorylation of AurA, induce mitotic arrest and apoptosis. LY3295668 erbumine avoids the formation of polyploids related to AurB inhibition. LY3295668 erbumine can be used for the study of small cell lung cancer.
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MK-5108-NH-PEG2-alkyne
0 ImagesCat. No.: HY-175827MK-5108-NH-PEG2-alkyne is a Aurora kinase A (AURKA) inhibitor. MK-5108-NH-PEG2-alkyne can be used for synthesis of PROTAC AURKA degrader 1 (HY-175830).
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SAR156497
0 ImagesCat. No.: HY-12476CAS No.: 1256137-14-0SAR156497 (compound 47) is an Aurora inhibitor, with IC50 values of 0.6 nM and 1 nM for Aurora A and Aurora B, respectively. SAR156497 can also inhibit PDE3, with IC50 value of 4 μM. SAR156497 can be used in anticancer research.
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TAK-901 hydrochloride
0 ImagesCat. No.: HY-12201ACAS No.: 934542-50-4TAK-901 hydrochloride is a multi-targeted aurora inhibitor with IC50s of 21 and 15 nM for aurora A and B, respectively.
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PROTAC Aurora A Degrader-1
0 ImagesCat. No.: HY-181568CAS No.: 3115344-59-4PROTAC Aurora A Degrader-1 is an orally active and blood-brain barrier-permeable selective Aurora A PROTAC degrader. PROTAC Aurora A Degrader-1 induces AURKA degradation with a DC50 of 6 nM in IMR32 cells (Dmax = 95%), eliminates both the kinase catalytic activity and N-Myc stabilizing scaffolding function of Aurora A, induces DNA damage, G2/M arrest and apoptosis, and shows antiproliferative activity. PROTAC Aurora A Degrader-1 is applicable to the research of neuroblastoma and small cell lung cancer.
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TDI6245
0 ImagesCat. No.: HY-187442TDI6245 is a Aurora kinase A (AURKA) inhibitor with an IC50 value of 21.64 nM against AURKA. TDI6245 also inhibits the β5 subunit of the 20S proteasome from Plasmodium falciparum (Pf 20S), with IC50 values of 0.11 μM, 31.1 μM and 6.8 μM against Pf 20S β5, human constitutive proteasome β5c and human immunoproteasome β5i subunits, respectively. TDI6245 binds to the AURKA pocket and the substrate cleft of Pf 20S β5 via antiparallel β-sheets and hydrogen bonds. TDI6245 inhibits the growth of Plasmodium falciparum. TDI6245 can be used in research related to triple-negative breast cancer and malaria.
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PF 477736 (Standard)
0 ImagesCat. No.: HY-10032RCAS No.: 952021-60-2Synonyms: PF 00477736 (Standard)PF 477736 (PF 00477736) (Standard) is the analytical standard of PF 477736 (HY-10032). This product is intended for research and analytical applications. PF 477736 (PF 00477736) is a potent, selective and ATP-competitive inhibitor of Chk1, with a Ki of 0.49 nM, it is also a Chk2 inhibitor, with a Ki of 47 nM. PF 477736 shows <100-fold selectivity for Chk1 over VEGFR2, Fms, Yes, Aurora-A, FGFR3, Flt3, and Ret (IC50=8 (Ki), 10, 14, 23, 23, 25, and 39 nM, respectively). PF 477736 can enhance Gemcitabine antitumor activity in vitro and in vivo.
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BPR1K653 hydrochloride
0 ImagesCat. No.: HY-120534CAS No.: 1192754-07-6BPR1K653 hydrochloride is a pan-Aurora kinase inhibitor, with an IC50 of 124.0 nM against Aurora-A and an IC50 of 45.0 nM against Aurora-B. BPR1K653 hydrochloride induces endoreduplication, apoptosis and antiproliferative activity in cancer cells. BPR1K653 hydrochloride can be used in research related to colon cancer and multidrug-resistant cancers.
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NEU-1953
0 ImagesCat. No.: HY-124633CAS No.: 2218480-85-2
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Benzo[c][1,8]naphthyridin-6(5H)-one
![Benzo[c][1,8]naphthyridin-6(5H)-one](https://file.medchemexpress.com/product_pic/hy-115862.gif "Click to View Benzo[c][1,8]naphthyridin-6(5H)-one Product Detail")
0 ImagesCat. No.: HY-115862CAS No.: 53439-81-9Benzo[c][1,8]naphthyridin-6(5H)-one exhibits low micromolar affinity to human adenosine receptor (AR) A1 and hA2A, with Ki of 4.6 and 4.8 μM. Benzo[c][1,8]naphthyridin-6(5H)-one is inhibitor for poly ADP-ribose polymerase-1 (PARP-1) and aurora kinase A, with IC50 of 0.311 and 5.5 μM.
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TY-011
0 ImagesCat. No.: HY-W395613CAS No.: 1389439-77-3TY-011 is an Aurora A/B kinase inhibitor. TY-011 induces abnormal microtubule-kinetochore attachment, leading to DNA damage and apoptosis (Apoptosis) in human gastric cancer cells, and ultimately inhibits cancer cell proliferation, with an IC50 value ranging from 0.11 to 4.49 μM in human gastric cancer cell lines. TY-011 has potential applications in gastric cancer research.
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Aurora A inhibitor 4
0 ImagesCat. No.: HY-169735CAS No.: 371224-09-8Aurora A inhibitor 4 (compound C9) is a potent inhibitor of Aurora A, with the GI50 of 4.26 and 7.08 μM in DU 145 cells and HT-29 cells, respectively.
