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]
-
Aurora A Related Products (114)
Related Products (114)
-
Antibodies (2)
-
JB170
0 ImagesJB170 is a potent and highly specific PROTAC-mediated AURORA-A (Aurora Kinase) degrader (DC50=28 nM) by linking Alisertib, to the Cereblon-binding molecule Thalidomide. JB170 preferentially binds AURORA-A (EC50=193 nM) over AURORA-B (EC50=1.4 µM). JB170-mediated S-phase arrest is caused specifically by AURORA-A depletion. JB170 has excellent ability to inhibit non-catalytic function of AURORA-A kinase.
-
Tinengotinib
0 ImagesSynonyms: TT 00420Tinengotinib (TT00420) is an orally active, spectrally selective small molecule kinase inhibitor targeting Aurora A/B (IC50=1.2-3.3 nM), FGFR1/2/3 (IC50=1.5-3.5 nM), VEGFRs, JAK1/2 and CSF1R. Tinengotinib blocks Aurora kinase-mediated cell cycle progression (inducing G2/M arrest), inhibits FGFR/JNK-JUN signaling pathway and activates MEK/ERK-dependent apoptotic pathway. Tinengotinib has the activity of anti-tumor proliferation, inducing apoptosis, inhibiting angiogenesis and regulating tumor microenvironment. Tinengotinib can be used in the study of triple-negative breast cancer (TNBC), gallbladder cancer and tumor immune microenvironment.
-
GRK6/Aurora A-IN-1
0 ImagesGRK6/Aurora A-IN-1 is a dual inhibitor of G protein-coupled receptor kinase 6 (GRK6)/Aurora A, with IC50 values of 120 nM and 11 nM, respectively. GRK6 is a key kinase required for the survival of multiple myeloma (MM) cells. GRK6-IN-2 has the potential for research on multiple myeloma.
-
CAM2602
0 ImagesCAM2602 is an orally active Aurora A-TPX2 protein−protein interaction inhibitor with a human Kd of 19 nM for Aurora A. CAM2602 increases the proportion of PH3 positive cells while reducing P-T288 Aurora A levels. CAM2602 arrests tumor xenograft growth in mice. CAM2602 can be used for the research of cancer, such as acute T cell leukemia.
-
GW779439X
0 ImagesGW779439X is a pyrazolopyridazine identified in an inhibitor of the S. aureus PASTA kinase Stk1. GW779439X potentiates the activity of β-lactam antibiotics against various MRSA and MSSA isolates, some even crossing the breakpoint from resistant to sensitive. GW779439X is an AURKA inhibitor and induces apoptosis by the caspases 3/7 pathway. MRSA:methicillin-resistant S. aureus; MSSA: methicillin-sensitive S. aureus
-
Cenisertib
0 ImagesSynonyms: AS-703569; R-763Cenisertib (AS-703569) is an ATP-competitive multi-kinase inhibitor that blocks the activity of Aurora-kinase-A/B, ABL1, AKT, STAT5 and FLT3. Cenisertib induces major growth-inhibitory effects by blocking the activity of several different molecular targets in neoplastic mast cells (MC). Cenisertib inhibits tumor growth in xenograft models of pancreatic, breast, colon, ovarian, and lung tumors and leukemia.
-
JAB-2485
0 ImagesJAB-2485 is an orally active and selective Aurora kinase A (AURKA) inhibitor with an IC50 value of 0.327 nM. JAB-2485 exhibits inhibitory activity against various tumor cell lines such as neuroblastoma, triple-negative breast cancer, small cell lung cancer, and epithelial ovarian cancer. JAB-2485 can induce cell cycle arrest and apoptosis in tumor cells. JAB-2485 has antitumor activity.
-
dAurAB5
0 ImagesdAurAB5 is a potent Aurora-A/Aurora-B PROTAC degrader with DC50 values of 8.8 nM and 6.1 nM, respectively. dAurAB5 promotes proteasomal degradation of target proteins, induces ubiquitination of Aurora-A and Aurora-B kinases, and downregulates the protein levels of TTK and MYCN. dAurAB5 can be used in studies related to neuroblastoma[1].
-
SK2188
0 ImagesSynonyms: JB325SK2188 (JB325) is a selective AURKA PROTAC degrader with a DC50 of 3.9 nM. SK2188 recruits CRBN E3 ubiquitin ligase to target and degrade AURKA, abrogating both its catalytic and non-kinase functions, which leads to the destabilization and degradation of the oncogenic protein MYCN, ultimately inducing replication stress, DNA damage and apoptosis. SK2188 is applicable to research related to neuroblastoma.
-
Ilorasertib
0 ImagesSynonyms: ABT-348Ilorasertib (ABT-348) 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 also is a potent VEGF, PDGF inhibitor. Ilorasertib has the potential for the research of acute myeloid leukemia (AML) and myelodysplastic syndrome (MDS).
-
SK2187
0 ImagesCat. No.: HY-171768CAS No.: 3038446-91-9Synonyms: JB301SK2187 (JB301) is a selective AURKA PROTAC degrader. SK2187 induces targeted degradation of AURKA by recruiting the CRBN E3 ubiquitin ligase. SK2187 is applicable to research related to neuroblastoma.
-
SP-96
0 ImagesSP-96 is a highly potent, selective and non-ATP-competitive Aurora B (IC50=0.316 nM) inhibitor and shows >2000 fold selectivity against FLT3 and KIT. SP-96 shows selective growth inhibition in NCI60 screening, incluing MDA-MD-468 (GI50=107 nM). SP-96 can be used for the research of triple negative breast cancer (TNBC).
