Aurora Kinase
Aurora kinases are highly conserved serine/threonine kinases that regulate mitotic progression and maintain chromosomal stability during cell division.[1][2] The mammalian Aurora kinase family comprises AURKA, AURKB, and AURKC, which share a conserved catalytic domain but differ in subcellular localization, substrate specificity, and mitotic function.[1][3] Mechanistically, AURKA controls centrosome maturation, spindle assembly, and G2/M transition, whereas AURKB functions as a chromosomal passenger kinase that regulates chromosome segregation and cytokinesis.[2][3][4] AURKC exhibits overlapping functions with AURKB but is predominantly associated with meiotic processes and germ-cell development.[5] Dysregulated Aurora kinase expression promotes genomic instability, aneuploidy, and uncontrolled proliferation, and overexpression of AURKA or AURKB has been reported in multiple human malignancies.[1][2][6] Therefore, Aurora kinase signaling has emerged as a central pathway linking mitotic control to tumorigenesis and therapeutic resistance.[6][7] Compared with related isoforms, AURKA has received particular attention because of its roles in spindle organization, DNA replication, and synthetic lethal interactions with tumor suppressor pathways, supporting its application as a precision oncology target.[2] For experimental applications, selective and pan-Aurora kinase inhibitors have been developed to disrupt mitotic progression, induce polyploidy or apoptosis, and evaluate Aurora-dependent vulnerabilities in cancer models.[4][7]
Referencias:
- [1]. Bavetsias V, et al. Aurora Kinase Inhibitors: Current Status and Outlook. Front Oncol. 2015 Dec 21;5:278. [Content Brief]
- [2]. Mou PK, et al. Aurora kinase A, a synthetic lethal target for precision cancer medicine. Exp Mol Med. 2021 May;53(5):835-847. [Content Brief]
- [3]. Vats P, et al. Aurora kinases signaling in cancer: from molecular perception to targeted therapies. Mol Cancer. 2025 Jun 18;24(1):180. [Content Brief]
- [4]. Ali SR, et al. Nerve Density and Neuronal Biomarkers in Cancer. Cancers (Basel). 2022 Oct 1;14(19):4817. [Content Brief]
- [5]. Wikipedia.
- [6]. Chung S, et al. Aurora kinases, emerging critical targets for cancer treatment and related new therapeutic strategies. Bioorg Chem. 2025 Aug;163:108633. [Content Brief]
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Productos relacionados con Aurora Kinase (90)
Productos relacionados con (90)
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KHS101 hydrochloride
0 ImagesKHS101 is a blood-brain barrier-penetrant anticancer agent that primarily functions by inhibiting HSPD1 (IC50 = 14.4 μM) and TACC3 across different cellular backgrounds. KHS101 promotes the aggregation of HSPD1 with client proteins, destabilizes TACC3, and reduces the levels of TACC3, Aurora A and PLK1. KHS101 induces autophagy, apoptosis, cell cycle exit and neuronal differentiation; it suppresses cancer cell growth, motility, EMT and stemness; it also impairs mitochondrial bioenergetics and glycolysis in glioblastoma cells. KHS101 can be used in research related to glioblastoma multiforme and breast cancer.
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Aurkin A
0 ImagesAurkin A is an allosteric inhibitor for the interaction between Aurora A Kinase (also known also Aurka) and TPX2, through targeting the TPX2 binding sites with Kd of 3.77 μM. Aurkin A can disrupt polyploidy induced by Alisertib (HY-10971) and increase apoptosis of tumor cells. Aurkin A can be used in research on mitosis and cancer.
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Gossypin
0 ImagesGossypin is an orally active flavone isolated from Hibiscus vitifolius. Gossypin has antioxidant, antiinflammatory, anticancer, anticataract, antidiabetic, and hepatoprotective activities. Gossypin inhibits NF-κB and NF-κB-regulated gene expression. Gossypin inhibits AURKA and RSK2. Gossypin inhibits invasion and induces apoptosis. Gossypin can be used for gastric cancer study.
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HLB-0532259
0 ImagesHLB-0532259 is a Aurora-A/N-Myc PROTAC degrader, with a DC50 of 20.2 nM against Aurora-A in MCF-7 cells; its DC50 values against N-Myc are 179 nM in SK-N-BE (2) cells and 229 nM in Kelly cells, respectively. HLB-0532259 induces apoptosis (apoptosis) in MYCN-amplified neuroblastoma cells and inhibits tumor growth in mouse xenograft models. HLB-0532259 can be used for the research of neuroblastoma.
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Aurora kinase-IN-3
0 ImagesAurora kinase-IN-3 (Compound 15a) is an orally active AURKB inhibitor that elicits an AURKB-suppressive activity by disrupting the mitotic localization of AURKB, rather than inhibiting its phosphorylation of H3 at Ser10.
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DB0614
0 ImagesDB0614 is a PROTAC based on Cereblon ligand, which is a selective and potent targeted protein degrader of NEK9 inhibitor. DB0614 can degrade ABL1, ABL2, BLK, CDK11B, CDK4, CSK, EPHA3, FER, GAK, LIMK1, MAP3K20, MAP4K1, MAP4K2, MAP4K3, MAP4K5, MAPK14, MAPK7, MAPK8, MAPK9, MAPKAPK2, MAPKAPK3, NLK, PDIK1L, PTK2B, RIPK1, RPS6KA1, RPS6KA3, SIK2, SIK3, STK35, TNK2 and ULK1. DB0614 can be used for research of disease or disorder mediated by aberrant kinase activity.
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MKI-3
0 ImagesReferencia número: HY-182391No. CAS: 3084702-28-0MKI-3 is a selective microtubule-associated serine/threonine kinase-like (MASTL) inhibitor with an IC50 of 5.72 nM and a Kd of 1.89 nM. MKI-3 disrupts the MASTL-ENSA-Aurora A signaling axis. MKI-3 induces chromosomal instability, mitotic catastrophe and apoptosis (apoptosis) in cancer cells. MKI-3 is applicable to research related to triple-negative breast cancer.
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TACC3-IN-3
0 ImagesReferencia número: HY-186208No. CAS: 3115244-67-9TACC3-IN-3 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-3 inhibits the proliferation of triple-negative breast cancer cells. TACC3-IN-3 is applicable to triple-negative breast cancer research.\n
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CD532 hydrochloride
0 ImagesCD532 hydrochloride is a potent Aurora A kinase inhibitor with an IC50 of 45 nM. CD532 hydrochloride has the dual effect of blocking Aurora A kinase activity and driving degradation of MYCN. CD532 hydrochloride also can directly interact with AURKA and induces a global conformational shift. CD532 hydrochloride can be used for the research of cancer.
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AAPK-25
0 ImagesAAPK-25 is a potent and selective Aurora/PLK dual inhibitor with anti-tumor activity, which can cause mitotic delay and arrest cells in a prometaphase, reflecting by the biomarker histone H3Ser10 phosphorylation and followed by a surge in apoptosis. AAPK-25 targets Aurora-A, -B, and -C with Kd values ranging from 23-289 nM, as well as PLK-1, -2, and -3 with Kd values ranging from 55-456 nM.
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DBPR728
0 ImagesDBPR728 is an acyl prodrug of 6K465 that carries fewer hydrogen bond donors. 6K465 acts as an Aurora kinase inhibitor that destabilizes MYC family cancer proteins and has antitumor efficacy. DBPR728 has the potential to inhibit cancers that overexpress C-MYC and N-MYC, with a 10-fold increase in oral bioavailability compared to 6K465.
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EGFR/AURKB-IN-1
0 ImagesEGFR/AURKB-IN-1 (compound 7) is a dual-targeted EGFR/AURKB inhibitor, and inhibits the phpsphorylations of L858R EGFR and AURKB with IC50s of 0.07 and 1.1, respectively. EGFR/AURKB-IN-1 occupies the hydrophobic region I or the αC-helix out pocket of EGFR and the back pocket of AURKB, inhibiting the growth, division and metastasis of tumor cells, thus can be used for cancer research.
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MASTL/Aurora A-IN-1
0 ImagesMASTL/Aurora A-IN-1 (Compound MA4) is a dual inhibitor of MASTL and Aurora A kinases with IC50 values of 0.56 μM and 0.16 μM, respectively. MASTL/Aurora A-IN-1 has broad-spectrum anticancer activity and has potent anticancer activity against SR (leukemia), K-562 (leukemia), MDA-MB-435 (melanoma), MOLT-4 (leukemia), and SK-MEL-2 (melanoma) cell lines in NCI-60 cancer cell lines with GI50 values of 0.023, 0.032, 0.037, 0.044, and 0.051 μM, respectively. MASTL/Aurora A-IN-1 inhibits Aurora A and MASTL kinases, inducing cell cycle G2/M arrest, thereby inhibiting cancer cell proliferation. MASTL/Aurora A-IN-1 can be used in cancer research, especially for tumors with dysregulated mitosis.
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6K465
0 Images6K465 is a pyrimidine-based Aurora A (AURKA) inhibitor. 6K465 can reduce the levels of c-MYC and N-MYC oncoproteins, demonstrating anticancer activity.
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Ceftriaxone (Standard)
0 ImagesReferencia número: HY-B0712RNo. CAS: 73384-59-5Synonyms: Ro 13-9904 free acid (Standard)Ceftriaxone (Standard) is the analytical standard of Ceftriaxone. This product is intended for research and analytical applications. Ceftriaxone (Ro 13-9904 free acid) is a broad spectrum β-lactam third-generation cephalosporin antibiotic, which has good antibacterial activity against a variety of gram-negative and positive bacteria. Ceftriaxone is a covalent inhibitor of GSK3β with IC50 value of 0.78 μM. Ceftriaxone is an inhibitor of Aurora B. Ceftriaxone has anti-inflammatory, antitumor and antioxidant activities. Ceftriaxone can be used in the study of bacterial infections and meningitis[1][2][3][4][5][6][7].
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AURKB Human Pre-designed siRNA Set A
0 ImagesReferencia número: HY-RS01270AURKB Human Pre-designed siRNA Set A contains three designed siRNAs for AURKB gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
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Aurora kinase inhibitor-8
0 ImagesAurora kinase inhibitor-8 is a highly selective inhibitor of the Aurora kinases.
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Cenisertib (Standard)
0 ImagesSynonyms: AS-703569 (Standard); R-763 (Standard)Cenisertib (Standard) is the analytical standard of Cenisertib. This product is intended for research and analytical applications. Cenisertib (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.
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Barasertib dihydrochloride
0 ImagesReferencia número: HY-10127ANo. CAS: 722543-50-2Synonyms: AZD1152 dihydrochloride
