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    AZ 3146
    AZ 3146

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1628
    CAS #: 1124329-14-1Purity ≥98%

    Description: AZ3146 is a novel, potent and selective Mps1 inhibitor with IC50 of ~35 nM, it contributes to recruitment of CENP-E (kinesin-related motor protein), and is less potent to FAK, JNK1, JNK2, and Kit. AZ3146 was used to probe the role of Mps1's catalytic activity during mitosis. AZ3146 also inhibits FAK, JNK1, JNK2, KSP and Kit. In in vitro kinase assays, AZ3146 inhibited human Mps1Cat with an IC50 (50% inhibitory concentration) of ~35 nM. AZ3146 also efficiently inhibited autophosphorylation of full-length Mps1 immunoprecipitated from human cells. 

    References: J Cell Biol. 2010 Jul 12;190(1):25-34.

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    Molecular Weight (MW)452.55
    FormulaC24H32N6O3
    CAS No.1124329-14-1
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 28 mg/mL (61.9 mM)
    Water:<1 mg/mL
    Ethanol: 91 mg/mL (201.1 mM)
    Other info

    Chemical Name: 9-cyclopentyl-2-(2-methoxy-4-(1-methylpiperidin-4-yloxy)phenylamino)-7-methyl-7H-purin-8(9H)-one

    InChi Key: YUKWVHPTFRQHMF-UHFFFAOYSA-N

    InChi Code: InChI=1S/C24H32N6O3/c1-28-12-10-17(11-13-28)33-18-8-9-19(21(14-18)32-3)26-23-25-15-20-22(27-23)30(24(31)29(20)2)16-6-4-5-7-16/h8-9,14-17H,4-7,10-13H2,1-3H3,(H,25,26,27)

    SMILES Code: O=C1N(C)C2=CN=C(NC3=CC=C(OC4CCN(C)CC4)C=C3OC)N=C2N1C5CCCC5           

    SynonymsAZ3146; AZ 3146; AZ-3146


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    In Vitro

    In vitro activity: AZ3146 also inhibits FAK, JNK1, JNK2 and Kit. AZ3146 significantly inhibits phosphorylation of Mps1 in cells. Mitotic-specific phospho forms of aurora B and BubR1 are not affected by AZ3146. AZ3146 does not inhibit Cdk1 or aurora B in mitotic cells. HeLa cells treated with nocodazole and 2 μM AZ3146 only delay mitosis briefly and then rereplicate their genomes, indicating that AZ3146 overrides the SAC. AZ3146 also inhibits an already established SAC signal, as after release from a nocodazole block, AZ3146 dramatically accelerates mitotic exit.During an otherwise unperturbed mitosis, AZ3146 reduces the time to complete mitosis from 90 minutes in controls to 32 minutes. Strikingly, ~90% of AZ3146-treated HeLa cells undergo abnormal mitoses, although ~50% enter anaphase without aligning all of their chromosomes, and ~30% exit mitosis without undergoing obvious chromosome segregation. AZ3146 has a dramatic effect on kinetochore localization of Mad2, reducing its levels to ~15%, but its effect on Mad1 is less pronounced, with levels remaining at ~60%. When Mps1 is inhibited by AZ3146 before mitotic entry, subsequent recruitment of Mad1 and Mad2 to kinetochores is abolished. However, if Mps1 is inhibited by AZ3146 after mitotic entry, the Mad1–C-Mad2 core complex remains kinetochore bound, but O-Mad2 is not recruited to the core.


    Kinase Assay: His-tagged human Mps1Cat encoding amino acids 510-857 is generated. For kinase assays, 500 ng is added to buffer (25 mM Tris-HCl, pH 7.4, 100 mM NaCl, 50 µg/mL BSA, 0.1 mM EGTA, 0.1% β-mercaptoethanol, 10 mM MgCl2, and 0.5 µg/mL myelin basic protein), AZ3146, and 100 µM γ-[32P]ATP (2 µCi/assay). Reactions are incubated at 30°C for 20 min, spotted onto P81 paper, washed in 0.5% phosphoric acid, and immersed in acetone. Phosphate incorporation is determined by scintillation counting. For immunoprecipitation kinase assays, HeLa cells are treated with nocodazole for 14 h, mitotic cells isolated, washed in PBS, and lysed for 30 min in 50 mM Tris-HCl, pH 7.4, 100 mM NaCl, 0.5% NP-40, 5 mM EDTA, 5 mM EGTA, 40 mM β-glycerophosphate, 0.2 mM PMSF, 1 mM DTT, 1 mM sodium orthovanadate, 20 mM sodium fluoride, 1 µM okadaic acid, and complete EDTA-free protease inhibitor cocktail. Full-length Mps1 is immunoprecipitated. Purified complexes are washed with lysis buffer containing 100 mM NaCl and assayed as described for the recombinant protein. To quantify 32P incorporation, reactions are stopped with SDS sample buffer and separated by SDS-PAGE followed by phosphorimaging. The plate is analyzed using a phosphorimager using AIDA software. To assess the specificity of AZ3146, a single-point screen is carried using kinase profiling service. 50 kinases are selected and assayed with 1 µM AZ3146


    Cell Assay: In cellular culture, if Mps1 is inhibited by AZ3146 before mitotic entry, this inhibition abloshed the subsequent recruitment of Mad1 and Mad2 to kinetochores. However, if cells were treated with AZ3146 after mitotic entry, the Mad1-C-Mad2 core complex remains kinetochore bound, but O-Mad2 is not recruited to the core. , AZ3146 interferes with chromosome alignment and overrides spindle assembly checkpoint1.

    In VivoRegarding the effect of AZ3146 administration in vivo, the evidence should be provided by performing the study in human or mice or other animal models.
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    References

    J Cell Biol. 2010 Jul 12;190(1):25-34.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    AZ 3146

    AZ3146, a novel Mps1 inhibitor. J Cell Biol. 2010 Jul 12;190(1):25-34.
     

    AZ 3146

    AZ3146 inhibits kinetochore recruitment of O-Mad2. J Cell Biol. 2010 Jul 12;190(1):25-34.
     

    AZ 3146

    AZ3146 enhances kinetochore localization of Mps1. J Cell Biol. 2010 Jul 12;190(1):25-34.


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