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Sotrastaurin

Cat. No.:YN310065

  • CAS No. :425637-18-9

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    • 产品名称: Sotrastaurin
      CAS No.: 425637-18-9
      Chemical Name: 3-(1H-indol-3-yl)-4-[2-(4-methyl-1-piperazinyl)-4-quinazolinyl]-1H-pyrrole-2,5-dione
      Synonyms:AEB071
      分子量:438.48
      分子式:C₂₅H₂₂N₆O₂
      SMILES:O=C(C(C1=C2C=CC=CC2=NC(N3CCN(C)CC3)=N1)=C4C5=CNC6=C5C=CC=C6)NC4=O
      存储:Please store the product under the recommended conditions in theCertificate of Analysis.
      运输:Room temperature in continental US; may vary elsewhere.
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      Purity: 98%
    • 产品描述: Sotrastaurin (AEB071) 是一种口服有效的 pan-PKC抑制剂,作用于 PKCθ,PKCβ,PKCα,PKCη,PKCδ 和 PKCε,Ki分别为 0.22 nM,0.64 nM,0.95 nM,1.8 nM,2.1 nM 和 3.2 nM。
      IC50和靶点: [{name:"PKCθ:0.22 nM (Ki)"},{name: "PKCβI:0.64 nM (Ki)"},{name: "PKCα:0.95 nM (Ki)"},{name: "PKCη:1.8 nM (Ki)"},{name: "PKCδ:2.1 nM (Ki)"},{name: "PKCε:3.2 nM (Ki)"}]
      In Vitro:
      In Vivo:
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    • Evenou, J.P., Wagner, J., Zenke, G., et al.The potent protein kinase C-selective inhibitor AEB071 (sotrastaurin) represents a new class of immunosuppressive agents affecting early T-cell activationJ. Pharmacol. Exp. Ther.330(3),792-801(2009)

      Vafadari, R., Kraaijeveld, R., Weimar, W., et al.Tacrolimus inhibits NF-κB activation in peripheral human T cellsPLoS One8(4),e60784(2014)

      Skvara, H., Dawid, M., Kleyn, E., et al.The PKC inhibitor AEB071 may be a therapeutic option for psoriasisJ. Clin. Invest.118(9),3151-3159(2008)

      Hardinger, K.L., and Brennan, D.C.Novel immunosuppressive agents in kidney transplantationWorld J. Transplant.3(4),68-77(2013)

      Verkaar, F., Blankesteijn, W.M., Smits, J.F.M., et al.β-Galactosidase enzyme fragment complementation for the measurement of Wnt/β-catenin signalingFASEB J.24(4),1205-1217(2010)

      Verkaar, F., van der Stelt, M., Blankesteijn, W.M., et al.Discovery of novel small molecule activators of β-catenin signalingPLoS One6(4),e19185(2011)

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