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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PROTAC AURKA degrader 3
0 ImagesCat. No.: HY-168543Purity: 99.78%PROTAC AURKA degrader 3 is a selective AURKA PROTAC degrader, with DC50 values of 2.05, 157.85 and 43.05 nM against AURKA, AURKB and TTK, respectively. PROTAC AURKA degrader 3 exhibits cytotoxicity against acute myeloid leukemia cells. PROTAC AURKA degrader 3 can be used for research related to acute myeloid leukemia.
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dAURK-4 hydrochloride
0 ImagesCat. No.: HY-137344APurity: 99.57%dAURK-4 hydrochloride is a selective AURKA PROTAC degrader. dAURK-4 hydrochloride promotes ubiquitination and degradation of AURKA. dAURK-4 hydrochloride can be used in the research of glioblastoma and multiple myeloma.
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Ilorasertib hydrochloride
0 ImagesSynonyms: ABT-348 hydrochlorideIlorasertib (ABT-348) hydrochloride is a potent, orally active and ATP-competitive aurora inhibitor with IC50s of116, 5, 1 nM for aurora A, aurora B, aurora C, respectively. Ilorasertib hydrochloride also is a potent VEGF, PDGF inhibitor. Ilorasertib hydrochloride has the potential for the research of acute myeloid leukemia (AML) and myelodysplastic syndrome (MDS).
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Aurora kinase inhibitor-3
0 ImagesAurora kinase inhibitor-3 is a strong and selective Aurora A kinase inhibitor with an IC50 of 42 nM, and weakly inhibits EGFR with an IC50 of >10 μM. Aurora kinase inhibitor-3 has a binding mode with the cyclopropanecarboxylic acid moiety directed towards the solvent exposed region of the ATP-binding pocket.
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Aurora kinase inhibitor-2
0 ImagesAurora kinase inhibitor-2 is a selective and ATP-competitive Aurora kinase inhibitor with IC50s of 310 nM and 240 nM for Aurora A and Aurora B, respectively.
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GSK2646264
0 ImagesGSK2646264 (Compound 44) is a potent and selective spleen tyrosine kinase (SYK) inhibitor with a pIC50 of 7.1. GSK2646264 also inhibits other kinases with pIC50 values of 5.4, 5.4, 5.3, 5, 4.5, <4.6 and <4.3 against LCK, LRRK2, GSK3β, JAK2, VEGFR2, Aurora B and Aurora A, respectively. GSK2646264 is penetrable into the epidermis and dermis of the skin.
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CCT400028
0 ImagesCat. No.: HY-181311Purity: 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.
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AurAP14
0 ImagesAurAP14 is an Aurora A PROTAC degrader (DC50 = 120 nM). AurAP14 can form a stable ternary complex with Aurora A kinase and HSP90, recruiting cullin family E3 ubiquitin ligases and MDM2 to mediate the ubiquitination and proteasome degradation of Aurora A kinase. AurAP14 increases p53 levels and decreases C-MYC levels; AurAP14 induces Apoptosis. AurAP14 can be used in the study of non-small cell lung cancer.
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SF-1
0 ImagesCat. No.: HY-168545Purity: 99.50%SF-1 is an AURKA ligand that can be used for the synthesis of PROTACs, such as PROTAC MPS1 degrader 2 (HY-168543). SF-1 can act as a free inhibitor and has the ability to pull down AURKA, AURKB, and TTK with DC50 values of 273.5, 933.5, and 1274 nM respectively. SF-1 has an anti-proliferative effect on acute myeloid leukemia.
