Aurora B
Aurora B (AURKB) is a mitotic serine/threonine kinase and the enzymatic core of the chromosomal passenger complex (CPC), which includes INCENP, Survivin, and Borealin[1]. Mechanistically, the CPC guides Aurora B through mitosis to control chromosome alignment, histone modification, kinetochore-microtubule error correction, spindle checkpoint signaling, and cytokinesis[1][2]. Therefore, Aurora B activity supports faithful chromosome segregation by releasing incorrect kinetochore-microtubule attachments, while reduced activity increases chromosome missegregation and aneuploid-cell generation[2]. In disease models, Aurora B deregulation or overexpression appears in several tumors, and studies in hepatocellular carcinoma, oral squamous cell carcinoma, prostate carcinoma, and glioblastoma connect Aurora B activity with recurrence, prognosis, tumor growth, or mitotic disruption[3][4][5][6]. Compared with related isoforms, Aurora A localizes to spindle poles and regulates mitotic entry, centrosome maturation, and spindle assembly, whereas Aurora B localizes with the CPC from inner centromeres to the spindle midzone and midbody[7]. Aurora C can act as a chromosomal passenger protein and complement Aurora B in mitotic cells, but Aurora B shows preferential INCENP binding and earlier M-phase expression[8]. For experimental applications, Aurora B or pan-Aurora inhibitors such as VX-680, AMG900, and danusertib help dissect metaphase-anaphase transition, cytokinetic initiation, mitotic progression, and cancer-cell proliferation[6][9][10].
Referencias:
- [1]. Vader G, et al. The chromosomal passenger complex: guiding Aurora-B through mitosis. J Cell Biol. 2006 Jun 19;173(6):833-7. [Content Brief]
- [2]. Abe Y, et al. System-level deficiencies in Aurora B control in cancers. Cell Cycle. 2016 Aug 17;15(16):2091-2092. [Content Brief]
- [3]. Tanaka S, et al. Aurora kinase B is a predictive factor for the aggressive recurrence of hepatocellular carcinoma after curative hepatectomy. Br J Surg. 2008 May;95(5):611-9. [Content Brief]
- [4]. Pannone G, et al. Aurora B expression as a prognostic indicator and possible therapeutic target in oral squamous cell carcinoma. Int J Immunopathol Pharmacol. 2011 Jan-Mar;24(1):79-88. [Content Brief]
- [5]. Cao M, et al. A Vector-Based Short Hairpin RNA Targeting Aurora B Suppresses Human Prostatic Carcinoma Growth. Technol Cancer Res Treat. 2017 Feb;16(1):112-119. [Content Brief]
- [6]. Ryu J, et al. An Aurora kinase inhibitor, AMG900, inhibits glioblastoma cell proliferation by disrupting mitotic progression. Cancer Med. 2018 Nov;7(11):5589-5603. [Content Brief]
- [7]. 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]
- [8]. Sasai K, et al. Aurora-C kinase is a novel chromosomal passenger protein that can complement Aurora-B kinase function in mitotic cells. Cell Motil Cytoskeleton. 2004 Dec;59(4):249-63. [Content Brief]
- [9]. Li Z, et al. The Aurora Kinase in Trypanosoma brucei plays distinctive roles in metaphase-anaphase transition and cytokinetic initiation. PLoS Pathog. 2009 Sep;5(9):e1000575. [Content Brief]
- [10]. Meulenbeld HJ, et al. Danusertib, an aurora kinase inhibitor. Expert Opin Investig Drugs. 2012 Mar;21(3):383-93. [Content Brief]
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Productos relacionados con Aurora B (80)
Productos relacionados con (80)
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Antibodies (1)
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RET-IN-19
0 ImagesReferencia número: HY-151377No. CAS: 2484919-71-1RET-IN-19 (compound 59) is a potent RET inhibitor, with IC50 values of 6.8 and 13.51 nM against RET-wt and RET V804M, respectively. RET-IN-19 shows anticancer activity. RET-IN-19 can be used for non-small cell lung cancer (NSCLC) research.
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SNS-314
0 ImagesReferencia número: HY-108344No. CAS: 1057249-41-8SNS-314 is a potent and selective aurora kinase inhibitor with IC50s of 9, 31, and 6 nM for aurora A, B and C, respectively.
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Aurora kinase inhibitor-10
0 ImagesReferencia número: HY-147993No. CAS: 2417228-90-9Aurora kinase inhibitor-10 (Compound 6c) is an orally active Aurora B inhibitor with an IC50 of 8 nM. Aurora kinase inhibitor-10 shows antitumor activity.
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Aurora kinase-IN-15
0 ImagesReferencia número: HY-184386Aurora kinase-IN-15 is a potent dual Aurora A and Aurora B kinase inhibitor. Aurora kinase-IN-15 has broad-spectrum anticancer activity and low toxicity to normal cells. Aurora kinase-IN-15 induces G2/M phase arrest, apoptosis, and activates the intrinsic apoptotic pathway through upregulation of Caspase 3 and Bax, along with downregulation of Bcl-2. Aurora kinase-IN-15 can be used for the study of breast cancer, hepatocellular carcinoma, colorectal cancer and prostate cancer.
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XMD-12
0 ImagesXMD-12 (compound 1) is an Aurora kinase (Aurora Kinase) inhibitor with anti-tumor activity that promotes paclitaxel (HY-B0015) induced cell death. XMD-12 exhibits high selectivity and potency against Aurora A, B, and C kinases, with IC50 values of 5.6, 18.4, and 24.6 nM, respectively.
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M9101
0 ImagesReferencia número: HY-184193M9101 is a selective Aurora A PROTAC degrader with a DC50 of 2.3 nM. M9101 induces G2/M arrest in triple-negative breast cancer cells and potently inhibits the proliferation of multiple tumor cell lines. M9101 can be used in the research of various cancers including triple-negative breast cancer.
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Aurora B/RET-IN-1
0 ImagesReferencia número: HY-189295Aurora B/RET-IN-1 is a dual RET and Aurora B inhibitor with human IC50 values of 78 nM and 24 nM, respectively. Aurora B/RET-IN-1 binds the DFG-out conformation of RET as a type II inhibitor and extends into the allosteric pocket. Aurora B/RET-IN-1 inhibits Aurora B kinase activity. Aurora B/RET-IN-1 inhibits RET and Aurora B signaling pathways. Aurora B/RET-IN-1 can be used for research on non-small cell lung cancer.
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Butrin
0 ImagesButrin is a compound found in Butea monosperma flowers. Butrin reduces expression of SIRT1, AURKB, cyclin D1, pAKT, GSK-3β, β-catenin, and TGF-3β expression, enhances apoptosis and ROS production in cancer cells. Butrin downregulates Wnt and NF-κB signaling, mitigates oxidative stress, reduces proinflammatory cytokine (TNF-α, IL-6 and IL-8) production and suppresses neuroinflammation. Butrin inhibits IKK enzyme activity. Butrin can be used for the researches of colorectal cancer, Alzheimer’s disease, and rheumatoid arthritis.
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Aurora kinase-IN-2
0 ImagesReferencia número: HY-150592No. CAS: 2241914-86-1Aurora kinase-IN-2 (compound 12Aj) is a potent Aurora kinase inhibitor with IC50 values of 90 and 152 nM for Aurora A and Aurora B. Aurora kinase-IN-2 arrests cell cycle at G2/M phase by regulating cyclin B1 and cdc2. Aurora kinase-IN-2 can be used for cancer research.
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Aurora kinase inhibitor-9
0 ImagesReferencia número: HY-147703No. CAS: 2419107-09-6Aurora kinase inhibitor-9 (compound 9d) is a potent AURKA/B dual aurora kinase inhibitor with IC50s of 0.093, 0.09 µM for Aurora A, Aurora B, respectively. Aurora kinase inhibitor-9 shows broad spectrum anti-proliferative activity.
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BRD-7880
0 ImagesReferencia número: HY-123610No. CAS: 1456542-69-0BRD-7880 is a potent and highly specific inhibitor of Aurora Kinase B (AURKB) and Aurora Kinase C (AURKC), with IC50 values of 7 nM and 12 nM, respectively.
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Aurora kinase ligand-1
0 ImagesReferencia número: HY-175526No. CAS: 1907679-70-2Aurora kinase ligand-1 (Compound I-4) is an Aurora kinase B (AURKB) PROTAC ligand. Aurora kinase ligand-1 can be conjugated with E3 ligase Ligand (HY-112078) and linker to synthesize AURKB PROTAC degrader MS44 (HY-175525). MS44 can be used for cancer research.
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LY3295668 erbumine
0 ImagesReferencia número: HY-114258ANo. CAS: 1919888-07-5Synonyms: 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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PROTAC AURKB Degrader-1
0 ImagesReferencia número: HY-184329No. CAS: 3114874-73-3PROTAC AURKB Degrader-1 is a selective AURKB PROTAC degrader with a DC50 value of 0.6 nM. PROTAC AURKB Degrader-1 promotes ubiquitination and degradation of AURKB. PROTAC AURKB Degrader-1 downregulates the expression levels of chromosomal passenger complex components Borealin, INCENP, Survivin as well as the transcription factor YY1. PROTAC AURKB Degrader-1 induces G2/M phase arrest and triggers Apoptosis in cells. PROTAC AURKB Degrader-1 serves as a chemical probe for biological studies of the chromosomal passenger complex. PROTAC AURKB Degrader-1 can be used in research related to acute myeloid leukemia, colorectal cancer, and non-small cell lung cancer.
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SAR156497
0 ImagesReferencia número: HY-12476No. CAS: 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 ImagesReferencia número: HY-12201ANo. CAS: 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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BPR1K653 hydrochloride
0 ImagesReferencia número: HY-120534No. CAS: 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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TY-011
0 ImagesReferencia número: HY-W395613No. CAS: 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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Binucleine 2
0 ImagesReferencia número: HY-121998No. CAS: 220088-42-6Binucleine 2 is an isoform-specific and ATP-competitive inhibitor of Drosophila Aurora B kinase (Ki=0.36 μM), a kinase involved in cell division. It is specific for Drosophila Aurora B kinase, inhibiting it in a dose-dependent manner, with minimal inhibition of human or X. laevis Aurora B kinases at concentrations up to 100 μM. Binucleine 2 induces mitotic and cytokinesis defects in Drosophila Kc167 cells. It prevents Drosophila S2 cells from assembling a contractile ring during cell division when used at a concentration of 40 μM but does not affect ring ingression, suggesting that Aurora B kinase activity is not required for that step.
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Aurora B inhibitor 1
0 ImagesReferencia número: HY-U00304No. CAS: 937276-52-3Aurora B inhibitor 1 is an Aurora B (Aurora-1) inhibitor extracted from patent WO2007059299A1, compound 1-3, has a Ki value of <0.010 uM.
