Chemical Name: 9-Cyclopentyl-2-[[2-methoxy-4-[(1-methylpiperidin-4-yl)oxy]-phenyl]amino]-7-methyl-7,9-dihydro-8H-purin-8-one
Biological ActivityAZ 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.
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.
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
Citations for AZ 3146
The citations listed below are publications that use Tocris products. Selected citations for AZ 3146 include:
8 Citations: Showing 1 - 8
Oncogenic MYC amplifies mitotic perturbations.
Authors: Littler Et al.
Open Biol 2019;9:190136
Cellular aspect ratio and cell division mechanics underlie the patterning of cell progeny in diverse mammalian epithelia.
Authors: McKinley Et al.
Chromosome Segregation Is Biased by Kinetochore Size.
Authors: Drpic Et al.
Curr Biol 2018;28:1344
Precocious centriole disengagement and centrosome fragmentation induced by mitotic delay.
Nat Commun 2017;8:15803
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
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
Cenp-E inhibitor GSK923295: Novel synthetic route and use as a tool to generate aneuploidy.
Authors: Bennett Et al.
Toxins (Basel) 2015;6:20921
Amitozyn impairs chromosome segregation and induces apoptosis via mitotic checkpoint activation.
Authors: Hermant Et al.
PLoS One 2013;8:e57461
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