Chemical Name: N-[4-[[6-Methoxy-7-[3-(4-morpholinyl)propoxy]-4-quinazolinyl]amino]phenyl]benzamide
Biological ActivityNovel, selective ATP-competitive inhibitor of Aurora B kinase in vitro (IC50 values are 50, 250 and 1000 nM for Aurora B, C and A kinases respectively). Selective over a range of other kinases including cdk1 and PLK1 (IC50 > 10 μM). Inhibits cell division and displays selective toxicity towards proliferating tumor cells versus non-dividing cells.
The technical data provided above is for guidance only.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Aurora B couples chromosome alignment with anaphase by targeting BubR1, Mad2, and Cenp-E to kinetochores.
Ditchfield et al.
J.Cell Biol., 2003;161:267
Discovery of novel and potent thiazoloquinazolines as selective Aurora A and B kinase inhibitors.
Jung et al.
Validating Aurora B as an anti-cancer drug target.
Girdler et al.
J.Cell Sci., 2006;119:3664
Citations for ZM 447439
The citations listed below are publications that use Tocris products. Selected citations for ZM 447439 include:
49 Citations: Showing 1 - 10
Oncogenic MYC amplifies mitotic perturbations.
Authors: Littler Et al.
Open Biol 2019;9:190136
Spatiotemporal control of mitotic exit during anaphase by an aurora B-Cdk1 crosstalk.
Authors: Afonso Et al.
Interactions between N-terminal Modules in MPS1 Enable Spindle Checkpoint Silencing.
Authors: Pachis Et al.
Cell Rep 2019;26:2101
Lipid accumulation facilitates mitotic slippage-induced adaptation to anti-mitotic drug treatment.
Authors: Wong Et al.
Cell Death Discov 2018;4:109
Atypical Cadherin Dachsous1b Interacts with Ttc28 and Aurora B to Control Microtubule Dynamics in Embryonic Cleavages.
Authors: Chen Et al.
Dev Cell 2018;45:376
Dynamic kinetochore size regulation promotes microtubule capture and chromosome biorientation in mitosis.
Authors: Sacristan Et al.
Nat Cell Biol 2018;20:800
Mps1 kinase-dependent Sgo2 centromere localisation mediates cohesin protection in mouse oocyte meiosis I.
Authors: Yakoubi Et al.
Nat Commun 2017;8:694
Aurora-B kinase pathway controls the lateral to end-on conversion of kinetochore-microtubule attachments in human cells.
Nat Commun 2017;8(1):150
Distinct Roles of the Chromosomal Passenger Complex in the Detection of and Response to Errors in Kinetochore-Microtubule Attachment.
Authors: Haase Et al.
Dev Cell 2017;42:640
Haspin inhibition reveals functional differences of interchromatid axis-localized AURKB and AURKC.
Authors: Quartuccio Et al.
Mol Biol Cell 2017;28:2233
Ska3 Phosphorylated by Cdk1 Binds Ndc80 and Recruits Ska to Kinetochores to Promote Mitotic Progression.
Authors: Zhang Et al.
Curr Biol 2017;27:1477
Baculoviral delivery of CRISPR/Cas9 facilitates efficient genome editing in human cells.
Authors: Hindriksen Et al.
PLoS One 2017;12:e0179514
Kif4 Is Essential for Mouse Oocyte Meiosis.
Authors: Camlin Et al.
PLoS One 2017;12:e0170650
Aurora-A mediated histone H3 phosphorylation of threonine 118 controls condensin I and cohesin occupancy in mitosis.
Authors: Wike Et al.
Haspin kinase regulates microtubule-organizing center clustering and stability through Aurora kinase C in mouse oocytes.
Authors: Balboula Et al.
J Cell Sci 2016;129:3648
Stable kinetochore-microtubule attachment is sufficient to silence the spindle assembly checkpoint in human cells.
Authors: Tauchman Et al.
J Cell Sci 2015;6:10036
Mio depletion links mTOR regulation to Aurora A and Plk1 activation at mitotic centrosomes.
Authors: Platani Et al.
J Cell Biol 2015;210:45
Multiple assembly mechanisms anchor the KMN spindle checkpoint platform at human mitotic kinetochores.
Authors: Kim and Yu
J Cell Biol 2015;208:181
Phosphorylation of myosin II-interacting guanine nucleotide exchange factor (MyoGEF) at threonine 544 by aurora B kinase promotes the binding of polo-like kinase 1 to MyoGEF.
Authors: Wu Et al.
J Biol Chem 2014;289:7142
Centmitor-1, a novel acridinyl-acetohydrazide, possesses similar molecular interaction field and antimitotic cellular phenotype as rigosertib, on 01910.Na.
Authors: Mäki-Jouppila Et al.
Nat Commun 2014;13:1054
Selective disruption of aurora C kinase reveals distinct functions from aurora B kinase during meiosis in mouse oocytes.
Authors: Balboula and Schindler
PLoS Genet 2014;10:e1004194
Oocytes isolated from dairy cows with reduced ovarian reserve have a high frequency of aneuploidy and alterations in the localization of progesterone receptor membrane component 1 and aurora kinase B.
Authors: Luciano Et al.
Biol Reprod 2013;88:58
Aurora B spatially regulates EB3 phosphorylation to coordinate daughter cell adhesion with cytokinesis.
Authors: Ferreira Et al.
J Cell Biol 2013;201:709
Spatiotemporal organization of Aurora-B by APC/CCdh1 after mitosis coordinates cell spreading through FHOD1.
Authors: Floyd Et al.
Cell Cycle 2013;126:2845
In vivo FRET imaging revealed a regulatory role of RanGTP in kinetochore-microtubule attachments via Aurora B kinase.
Authors: Lee Et al.
PLoS One 2012;7:e45836
A cell cycle role for the epigenetic factor CTCF-L/BORIS.
Authors: Rosa-Garrido Et al.
PLoS One 2012;7:e39371
Haspin inhibitors reveal centromeric functions of Aurora B in chromosome segregation.
Authors: Wang Et al.
J Cell Biol 2012;199:251
Appearance and heterochromatin localization of HP1α in early mouse embryos depends on cytoplasmic clock and H3S10 phosphorylation.
Authors: Meglicki Et al.
Cell Cycle 2012;11:2189
The chromosomal passenger complex activates Polo kinase at centromeres.
Authors: Carmena Et al.
PLoS Biol 2012;10:e1001250
Quantitative phosphoproteomics identifies substrates and functional modules of Aurora and Polo-like kinase activities in mitotic cells.
Authors: Kettenbach Et al.
Sci Signal 2011;4:rs5
Aurora kinase B activity is modulated by thyroid hormone during transcriptional activation of pituitary genes.
Authors: Tardáguila Et al.
Mol Endocrinol 2011;25:385
Zwint-1 is a novel Aurora B substrate required for the assembly of a dynein-binding platform on kinetochores.
Authors: Kasuboski Et al.
Mol Biol Cell 2011;22:3318
Polo-box domain inhibitor poloxin activates the spindle assembly checkpoint and inhibits tumor growth in vivo.
Authors: Yuan Et al.
Am J Pathol 2011;179:2091
Formation of stable attachments between kinetochores and microtubules depends on the B56-PP2A phosphatase.
Authors: Foley Et al.
Nat Cell Biol 2011;13:1265
Role of a novel coiled-coil domain-containing protein CCDC69 in regulating central spindle assembly.
Authors: Pal Et al.
J Am Soc Nephrol 2010;9:4117
VHL inactivation induces HEF1 and Aurora kinase A.
Authors: Xu Et al.
J Cell Biol 2010;21:2041
Relocation of the chromosomal passenger complex prevents mitotic checkpoint engagement at anaphase.
Authors: Vázquez-Novelle and Petronczki
Curr Biol 2010;20:1402
Plk1 negatively regulates Cep55 recruitment to the midbody to ensure orderly abscission.
Authors: Bastos and Barr
J Cell Biol 2010;191:751
Release of Mps1 from kinetochores is crucial for timely anaphase onset.
Authors: Jelluma Et al.
Cell Cycle 2010;191:281
Epigenetic centromere specification directs aurora B accumulation but is insufficient to efficiently correct mitotic errors.
Authors: Bassett Et al.
Mol Cancer Ther 2010;190:177
Targeting mitotic exit leads to tumor regression in vivo: Modulation by Cdk1, Mastl, and the PP2A/B55α,δ phosphatase.
Authors: Manchado Et al.
Cancer Cell 2010;18:641
The Aurora kinase inhibitor ZM447439 accelerates first meiosis in mouse oocytes by overriding the spindle assembly checkpoint.
Authors: Lane Et al.
Human condensin function is essential for centromeric chromatin assembly and proper sister kinetochore orientation.
Authors: Samoshkin Et al.
PLoS One 2009;4:e6831
Discovery and exploitation of inhibitor-resistant aurora and polo kinase mutants for the analysis of mitotic networks.
Authors: Scutt Et al.
J Biol Chem 2009;284:15880
The Nup107-160 nucleoporin complex promotes mitotic events via control of the localization state of the chromosome passenger complex.
Authors: Platani Et al.
Mol Biol Cell 2009;20:5260
Cell cycle dependent degradation of MCAK: evidence against a role in anaphase chromosome movement.
Authors: Ganguly Et al.
Toxins (Basel) 2008;7:3187
A mitotic GlcNAcylation/phosphorylation signaling complex alters the posttranslational state of the cytoskeletal protein vimentin.
Authors: Slawson Et al.
Mol Biol Cell 2008;19:4130
Cancer cells display profound intra- and interline variation following prolonged exposure to antimitotic drugs.
Authors: Gascoigne and Taylor
Cancer Cell 2008;14:111
Frequent overexpression of aurora B kinase, a novel drug target, in non-small cell lung carcinoma patients.
Authors: Vischioni Et al.
Mol Cancer Ther 2006;5:2905
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The product was used to release the cells in mitosis after STLC clock