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Biological Activity for AZ 3146
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.
Sold for research purposes only under agreement from AstraZeneca UK Ltd.
Compound Libraries for AZ 3146
Technical Data for AZ 3146
|Storage||Store at +4°C|
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 Data for AZ 3146
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for AZ 3146
The following data is based on the product molecular weight 452.55. 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|
|0.75 mM||2.95 mL||14.73 mL||29.46 mL|
|3.75 mM||0.59 mL||2.95 mL||5.89 mL|
|7.5 mM||0.29 mL||1.47 mL||2.95 mL|
|37.5 mM||0.06 mL||0.29 mL||0.59 mL|
References for AZ 3146
References are publications that support the biological activity of the product.
Hewitt et al (2010) Sustained Mps1 activity is required in mitosis to recruit O-Mad2 to the Mad1-C-Mad2 core complex. J.Cell Biol. 190 25 PMID: 20624899
Lan and Cleveland (2010) A chemical tool box defines mitotic and interphase roles for Mps1 kinase. J.Cell.Biol. 190 21 PMID: 20624898
Maciejowski et al (2010) Mps1 directs the assembly of Cdc20 inhbitory complexes during interphase and mitosis to control M phase timing and spindle checkpoint signaling. J.Cell Biol. 190 89 PMID: 20624902
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Keywords: AZ 3146, AZ 3146 supplier, AZ, astrazeneca, Mps1, monopolar, spindle, selective, potent, inhibitors, inhibits, SAC, assembly, checkpoint, control, TTK, dual-specificity, protein, kinases, kinetochores, CENP-E, centromere, E, AZ3146, Checkpoint, Control, Kinases, Monopolar, Spindle, 1, Kinase, 3994, Tocris Bioscience
8 Citations for AZ 3146
Citations are publications that use Tocris products. Selected citations for AZ 3146 include:
Littler et al (2019) Oncogenic MYC amplifies mitotic perturbations. Open Biol 9 190136 PMID: 31455158
Karki (2017) Precocious centriole disengagement and centrosome fragmentation induced by mitotic delay. Nat Commun 8 15803 PMID: 28607478
Drpic et al (2018) Chromosome Segregation Is Biased by Kinetochore Size. Curr Biol 28 1344 PMID: 29706521
McKinley et al (2018) Cellular aspect ratio and cell division mechanics underlie the patterning of cell progeny in diverse mammalian epithelia. Elife 7 PMID: 29897330
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
Bennett et al (2015) Cenp-E inhibitor GSK923295: Novel synthetic route and use as a tool to generate aneuploidy. Toxins (Basel) 6 20921 PMID: 26320186
Hermant et al (2013) Amitozyn impairs chromosome segregation and induces apoptosis via mitotic checkpoint activation. PLoS One 8 e57461 PMID: 23505430
Garvanska et al (2016) Synergistic inhibition of the APC/C by the removal of APC15 in HCT116 cells lacking UBE2C. Biol Open 5 1441 PMID: 27591192
Do you know of a great paper that uses AZ 3146 from Tocris? Please let us know.
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Literature in this Area
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Cell Cycle & DNA Damage Repair Poster
In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.