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NMS-873,ATPaseVCP/p97Inhibitor M60165-2s|产品详情|进口橙子视频旧款采购网




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    NMS-873,ATPaseVCP/p97Inhibitor
    品牌:Xcessbio
    货号:M60165-2s
    规格:2mg solid
    货期:

    NMS-873,ATPaseVCP/p97Inhibitor

    商品详情 参考文献 相关资料
    Product Information
    Molecular Weight: 520.67
    Formula: C27H28N4O3S2
    Purity: ≥98%
    CAS#: 1418013-75-8
    Solubility: DMSO up to 100 mM
    Chemical Name: 3-(3-(cyclopentylthio)-5-(((2-methyl-4'-(methylsulfonyl)-[1,1'-biphenyl]-4-yl)oxy)methyl)-4H-1,2,4-triazol-4-yl)pyridine
    Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

    Biological Activity:

    NMS-873 is a potent and specific small molecule allosteric inhibitor of the ATPase VCP/p97 (IC50 ~0.03 µM), identified by a high-throughput screening. It is very selective (IC50 >10 μM) against all of the AAA ATPases, HSP90 or the 53 kinases tested. Using photo-affinity labeling, structural analysis and mutagenesis, the of NMS-873 was found to be a region spanning the D1 and D2 domains of adjacent protomers encompassing elements important for nucleotide-state sensing and ATP hydrolysis. NMS-873 activated the unfolded protein response, interfered with autophagy, and induced cancer cell death. NMS-873 provided critical validation of VCP as a cancer target, and it raises the possibility that targeting VCP might prevent proteasome inhibitor–resistant tumors from escaping through the aggresome-autophagy pathways and cause them to collapse under the high load of unfolded proteins. 

     

    How to Use:

    • In vitro:  NMS-873 was used at 2.5-10 µM final concentration in various in vitro assays. 
    • In vivo: n/a

     

    Reference:

    1. 1. Magnaghi P, et al. Covalent and allosteric inhibitors of the ATPase VCP/p97 induce cancer cell death. (2013) Nat Chem Biol. 9(9):548-56
     

     

    Products are for research use only. Not for human use.

     

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