AZ 3146
Chemical Name: 9-Cyclopentyl-2-[[2-methoxy-4-[(1-methylpiperidin-4-yl)oxy]-phenyl]amino]-7-methyl-7,9-dihydro-8H-purin-8-one
Purity: ≥99%
Biological Activity
AZ 3146 is a potent and selective monopolar spindle 1 (Mps1) kinase inhibitor (IC50 = 35 nM). Displays selectivity over 46 other kinases including Cdk1 and aurora kinase B. Interferes with chromosome alignment and overrides spindle assembly checkpoint. Inhibits the recruitment of Mad1, Mad2 and centromere protein E (CENP-E) to kinetochores.Technical Data
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.
Additional Information
Background References
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Genome-wide transcriptome profiling of homologous recombination DNA repair.
Peng, Guang, Chun-Jen Lin, Curtis, Mo, Wei, Dai, Hui, Park, Yun-Yong, Kim, Soo Mi, Peng, Yang, Mo, Qianxing, Siwko, Stefan, Hu, Ruozhen, Lee, Ju-Seog, Hennessy, Bryan, Hanash, Samir, Mills, Gordon B, Lin, Shiaw-Yi
Nat Commun, 2014;5(0):3361. -
A chemical tool box defines mitotic and interphase roles for Mps1 kinase.
Lan and Cleveland
J.Cell Biol., 2010;190:21 -
Sustained Mps1 activity is required in mitosis to recruit O-Mad2 to the Mad1-C-Mad2 core complex.
Hewitt et al.
J.Cell Biol., 2010;190:25 -
Mps1 directs the assembly of Cdc20 inhbitory complexes during interphase and mitosis to control M phase timing and spindle checkpoint signaling.
Maciejowski et al.
J.Cell Biol., 2010;190:89
Product Datasheets
Citations for AZ 3146
The citations listed below are publications that use Tocris products. Selected citations for AZ 3146 include:
13 Citations: Showing 1 - 10
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Separase cleaves the kinetochore protein Meikin at the meiosis I/II transition.
Authors: Jun Et al.
Dev Cell 2021;56:2192-2206.e8
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Ordered dephosphorylation initiated by the selective proteolysis of cyclin B drives mitotic exit.
Authors: Shabaz Et al.
Elife 2020;9
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Small-molecule inhibition of aging-associated chromosomal instability delays cellular senescence.
Authors: Joana C Et al.
EMBO Rep 2020;21:e49248
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Oncogenic MYC amplifies mitotic perturbations.
Authors: Littler Et al.
Open Biol 2019;9:190136
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Cellular aspect ratio and cell division mechanics underlie the patterning of cell progeny in diverse mammalian epithelia.
Authors: McKinley Et al.
Elife 2018;7
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Chromosome Segregation Is Biased by Kinetochore Size.
Authors: Drpic Et al.
Curr Biol 2018;28:1344
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Methods for High-throughput Drug Combination Screening and Synergy Scoring.
Authors: Jing Et al.
Methods Mol Biol 2018;1711:351-398
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Precocious centriole disengagement and centrosome fragmentation induced by mitotic delay.
Authors: Karki
Nat Commun 2017;8:15803
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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
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Large-Scale Analysis of CRISPR/Cas9 Cell-Cycle Knockouts Reveals the Diversity of p53-Dependent Responses to Cell-Cycle Defects.
Authors: Iain M Et al.
Dev Cell 2017;40:405-420.e2
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Synergistic inhibition of the APC/C by the removal of APC15 in HCT116 cells lacking UBE2C.
Authors: Garvanska Et al.
Biol Open 2016;5:1441
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Cenp-E inhibitor GSK923295: Novel synthetic route and use as a tool to generate aneuploidy.
Authors: Bennett Et al.
Toxins (Basel) 2015;6:20921
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Amitozyn impairs chromosome segregation and induces apoptosis via mitotic checkpoint activation.
Authors: Hermant Et al.
PLoS One 2013;8:e57461
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