ZM 447439

Name: ZM 447439
Brand: Tocris Bioscience
SKU: 2458
Rating: 4 (1 reviews)

Tocris Bioscience a Bio-Techne Brand

Catalog # 2458

Citations (50)

(1)

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Key Product Details

Description:	Inhibits Aurora kinase B
Chemical Name:	N-[4-[[6-Methoxy-7-[3-(4-morpholinyl)propoxy]-4-quinazolinyl]amino]phenyl]benzamide
Purity:	≥98% (HPLC)
Molecular Weight:	513.59

View Full Technical Details for ZM 447439

Biological Activity for ZM 447439

ZM 447439 is a novel, 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.

Licensing Information

Sold with the permission of AstraZeneca UK Ltd.

Compound Libraries for ZM 447439

ZM 447439 is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library and Tocriscreen Epigenetics Library. Find out more about compound libraries available from Tocris.

Technical Data for ZM 447439

M. Wt	513.59
Formula	C₂₉H₃₁N₅O₄
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	331771-20-1
PubChem ID	9914412
InChi Key	OGNYUTNQZVRGMN-UHFFFAOYSA-N
Smiles	COC1=CC2=C(NC3=CC=C(NC(=O)C4=CC=CC=C4)C=C3)N=CN=C2C=C1OCCCN1CCOCC1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for ZM 447439

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	51.36	100

Preparing Stock Solutions for ZM 447439

The following data is based on the product molecular weight 513.59.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.95 mL	9.74 mL	19.47 mL
5 mM	0.39 mL	1.95 mL	3.89 mL
10 mM	0.19 mL	0.97 mL	1.95 mL
50 mM	0.04 mL	0.19 mL	0.39 mL

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References for ZM 447439

References are publications that support the biological activity of the product.

Jung Discovery of novel and potent thiazoloquinazolines as selective Aurora A and B kinase inhibitors. J.Med.Chem. 2006 PMID: 16451062
Girdler Validating Aurora B as an anti-cancer drug target. J.Cell Sci. 2006 PMID: 16912073
Ditchfield Aurora B couples chromosome alignment with anaphase by targeting BubR1, Mad2, and Cenp-E to kinetochores. J.Cell Biol. 2003 PMID: 12719470

Citations for ZM 447439 (50)

Showing 1 - 10 of 50 citations Showing All

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Citations are publications that use Bio-Techne products. Selected citations for ZM 447439 include:

Gulluni et al. (2021) PI(3,4)P2-mediated cytokinetic abscission prevents early senescence and cataract formation. Science. 374
PMID: 34882480
Littler et al. (2019) Oncogenic MYC amplifies mitotic perturbations. Open Biol. 9:190136
PMID: 31455158
Afonso et al. (2019) Spatiotemporal control of mitotic exit during anaphase by an aurora B-Cdk1 crosstalk. Elife. 8
PMID: 31424385
Pachis et al. (2019) Interactions between N-terminal Modules in MPS1 Enable Spindle Checkpoint Silencing. Cell Rep. 26:2101
PMID: 30784592
Wong et al. (2018) Lipid accumulation facilitates mitotic slippage-induced adaptation to anti-mitotic drug treatment. Cell Death Discov. 4:109
PMID: 30510774
Sacristan et al. (2018) Dynamic kinetochore size regulation promotes microtubule capture and chromosome biorientation in mitosis. Nat Cell Biol. 20:800
PMID: 29915359
Chen et al. (2018) Atypical Cadherin Dachsous1b Interacts with Ttc28 and Aurora B to Control Microtubule Dynamics in Embryonic Cleavages. Dev Cell. 45:376
PMID: 29738714
Shrestha (2017) Aurora-B kinase pathway controls the lateral to end-on conversion of kinetochore-microtubule attachments in human cells. Nat Commun. 8(1):150
PMID: 28751710
Hindriksen et al. (2017) Baculoviral delivery of CRISPR/Cas9 facilitates efficient genome editing in human cells. PLoS One. 12:e0179514
PMID: 28640891
Quartuccio et al. (2017) Haspin inhibition reveals functional differences of interchromatid axis-localized AURKB and AURKC. Mol Biol Cell. 28:2233
PMID: 28659416
Yakoubi et al. (2017) Mps1 kinase-dependent Sgo2 centromere localisation mediates cohesin protection in mouse oocyte meiosis I. Nat Commun. 8:694
PMID: 28947820
Camlin et al. (2017) Kif4 Is Essential for Mouse Oocyte Meiosis. PLoS One. 12:e0170650
PMID: 28125646
Zhang et al. (2017) Ska3 Phosphorylated by Cdk1 Binds Ndc80 and Recruits Ska to Kinetochores to Promote Mitotic Progression. Curr Biol. 27:1477
PMID: 28479321
Haase et al. (2017) Distinct Roles of the Chromosomal Passenger Complex in the Detection of and Response to Errors in Kinetochore-Microtubule Attachment. Dev Cell. 42:640
PMID: 28950102
Wike et al. (2016) Aurora-A mediated histone H3 phosphorylation of threonine 118 controls condensin I and cohesin occupancy in mitosis. Elife. 5:e11402
PMID: 26878753
Balboula et al. (2016) Haspin kinase regulates microtubule-organizing center clustering and stability through Aurora kinase C in mouse oocytes. J Cell Sci. 129:3648
PMID: 27562071
Kim and Yu (2015) Multiple assembly mechanisms anchor the KMN spindle checkpoint platform at human mitotic kinetochores. J Cell Biol. 208:181
PMID: 25601404
Platani et al. (2015) Mio depletion links mTOR regulation to Aurora A and Plk1 activation at mitotic centrosomes. J Cell Biol. 210:45
PMID: 26124292
Tauchman et al. (2015) Stable kinetochore-microtubule attachment is sufficient to silence the spindle assembly checkpoint in human cells. J Cell Sci. 6:10036
PMID: 26620470
Balboula and Schindler (2014) Selective disruption of aurora C kinase reveals distinct functions from aurora B kinase during meiosis in mouse oocytes. PLoS Genet. 10:e1004194
PMID: 24586209
Mäki-Jouppila et al. (2014) Centmitor-1, a novel acridinyl-acetohydrazide, possesses similar molecular interaction field and antimitotic cellular phenotype as rigosertib, on 01910.Na. Nat Commun. 13:1054
PMID: 24748653
Wu et al. (2014) 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. J Biol Chem. 289:7142
PMID: 24482237
Ferreira et al. (2013) Aurora B spatially regulates EB3 phosphorylation to coordinate daughter cell adhesion with cytokinesis. J Cell Biol. 201:709
PMID: 23712260
Floyd et al. (2013) Spatiotemporal organization of Aurora-B by APC/CCdh1 after mitosis coordinates cell spreading through FHOD1. Cell Cycle. 126:2845
PMID: 23613471
Luciano et al. (2013) 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. Biol Reprod. 88:58
PMID: 23325810
Wang et al. (2012) Haspin inhibitors reveal centromeric functions of Aurora B in chromosome segregation. J Cell Biol. 199:251
PMID: 23071152
Carmena et al. (2012) The chromosomal passenger complex activates Polo kinase at centromeres. PLoS Biol. 10:e1001250
PMID: 22291575
Lee et al. (2012) In vivo FRET imaging revealed a regulatory role of RanGTP in kinetochore-microtubule attachments via Aurora B kinase. PLoS One. 7:e45836
PMID: 23029267
Meglicki et al. (2012) Appearance and heterochromatin localization of HP1α in early mouse embryos depends on cytoplasmic clock and H3S10 phosphorylation. Cell Cycle. 11:2189
PMID: 22622086
Rosa-Garrido et al. (2012) A cell cycle role for the epigenetic factor CTCF-L/BORIS. PLoS One. 7:e39371
PMID: 22724006
Kasuboski et al. (2011) Zwint-1 is a novel Aurora B substrate required for the assembly of a dynein-binding platform on kinetochores. Mol Biol Cell. 22:3318
PMID: 21775627
Tardáguila et al. (2011) Aurora kinase B activity is modulated by thyroid hormone during transcriptional activation of pituitary genes. Mol Endocrinol. 25:385
PMID: 21239609
Yuan et al. (2011) Polo-box domain inhibitor poloxin activates the spindle assembly checkpoint and inhibits tumor growth in vivo. Am J Pathol. 179:2091
PMID: 21839059
Foley et al. (2011) Formation of stable attachments between kinetochores and microtubules depends on the B56-PP2A phosphatase. Nat Cell Biol. 13:1265
PMID: 21874008
Kettenbach et al. (2011) Quantitative phosphoproteomics identifies substrates and functional modules of Aurora and Polo-like kinase activities in mitotic cells. Sci Signal. 4:rs5
PMID: 21712546
Bastos and Barr (2010) Plk1 negatively regulates Cep55 recruitment to the midbody to ensure orderly abscission. J Cell Biol. 191:751
PMID: 21079244
Manchado et al. (2010) Targeting mitotic exit leads to tumor regression in vivo: Modulation by Cdk1, Mastl, and the PP2A/B55α,δ phosphatase. Cancer Cell. 18:641
PMID: 21156286
Vázquez-Novelle and Petronczki (2010) Relocation of the chromosomal passenger complex prevents mitotic checkpoint engagement at anaphase. Curr Biol. 20:1402
PMID: 20619651
Bassett et al. (2010) Epigenetic centromere specification directs aurora B accumulation but is insufficient to efficiently correct mitotic errors. Mol Cancer Ther. 190:177
PMID: 20643881
Pal et al. (2010) Role of a novel coiled-coil domain-containing protein CCDC69 in regulating central spindle assembly. J Am Soc Nephrol. 9:4117
PMID: 20962590
Xu et al. (2010) VHL inactivation induces HEF1 and Aurora kinase A. J Cell Biol. 21:2041
PMID: 20864688
Jelluma et al. (2010) Release of Mps1 from kinetochores is crucial for timely anaphase onset. Cell Cycle. 191:281
PMID: 20937696
Lane et al. (2010) The Aurora kinase inhibitor ZM447439 accelerates first meiosis in mouse oocytes by overriding the spindle assembly checkpoint. Reproduction. 140:521
PMID: 20660090
Scutt et al. (2009) Discovery and exploitation of inhibitor-resistant aurora and polo kinase mutants for the analysis of mitotic networks. J Biol Chem. 284:15880
PMID: 19359241
Platani et al. (2009) The Nup107-160 nucleoporin complex promotes mitotic events via control of the localization state of the chromosome passenger complex. Mol Biol Cell. 20:5260
PMID: 19864462
Samoshkin et al. (2009) Human condensin function is essential for centromeric chromatin assembly and proper sister kinetochore orientation. PLoS One. 4:e6831
PMID: 19714251
Slawson et al. (2008) A mitotic GlcNAcylation/phosphorylation signaling complex alters the posttranslational state of the cytoskeletal protein vimentin. Mol Biol Cell. 19:4130
PMID: 18653473
Ganguly et al. (2008) Cell cycle dependent degradation of MCAK: evidence against a role in anaphase chromosome movement. Toxins (Basel). 7:3187
PMID: 18843200
Gascoigne and Taylor (2008) Cancer cells display profound intra- and interline variation following prolonged exposure to antimitotic drugs. Cancer Cell. 14:111
PMID: 18656424
Vischioni et al. (2006) Frequent overexpression of aurora B kinase, a novel drug target, in non-small cell lung carcinoma patients. Mol Cancer Ther. 5:2905
PMID: 17121938

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ZM447439 releases cells into mitosis

Name: Valeria Marotta

Species: Human

Assay Type: In Vitro

Cell Line/Tissue: U2OS

The product was used to release the cells in mitosis after STLC clock

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