Home / TTK/Mps1 Kinase Inhibitors / AZ 3146

AZ 3146

Catalog #: 3994
13 Citations Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
3994/10
3994/50
AZ 3146 | CAS No. 1124329-14-1 | TTK/Mps1 Kinase Inhibitors
1 Image
Description: Potent and selective Mps1 kinase inhibitor

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%

Product Details
Citations (13)
Reviews
Biological Activity Technical Data Additional Information Background Product Datasheets Calculators

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

M.Wt:
452.55
Formula:
C24H32N6O3
Solubility:
Soluble to 25 mM in DMSO and to 75 mM in ethanol
Purity:
≥99%
Storage:
Store at +4°C
CAS No:
1124329-14-1

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

Licensing Caveats:
Sold for research purposes only under agreement from AstraZeneca UK Ltd.

Background References

  1. 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.
  2. A chemical tool box defines mitotic and interphase roles for Mps1 kinase.
    Lan and Cleveland
    J.Cell Biol., 2010;190:21
  3. 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
  4. 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

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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

  1. Separase cleaves the kinetochore protein Meikin at the meiosis I/II transition.
    Authors: Jun Et al.
    Dev Cell  2021;56:2192-2206.e8
  2. Ordered dephosphorylation initiated by the selective proteolysis of cyclin B drives mitotic exit.
    Authors: Shabaz Et al.
    Elife  2020;9
  3. Small-molecule inhibition of aging-associated chromosomal instability delays cellular senescence.
    Authors: Joana C Et al.
    EMBO Rep  2020;21:e49248
  4. Oncogenic MYC amplifies mitotic perturbations.
    Authors: Littler Et al.
    Open Biol  2019;9:190136
  5. Cellular aspect ratio and cell division mechanics underlie the patterning of cell progeny in diverse mammalian epithelia.
    Authors: McKinley Et al.
    Elife  2018;7
  6. Chromosome Segregation Is Biased by Kinetochore Size.
    Authors: Drpic Et al.
    Curr Biol  2018;28:1344
  7. Methods for High-throughput Drug Combination Screening and Synergy Scoring.
    Authors: Jing Et al.
    Methods Mol Biol  2018;1711:351-398
  8. Precocious centriole disengagement and centrosome fragmentation induced by mitotic delay.
    Authors: Karki
    Nat Commun  2017;8:15803
  9. 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
  10. 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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