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Rottlerin

Cat. No.:YN310314

  • CAS No. :82-08-6

    • 产品资料
    • 生物活性
    • 参考文献
    • 产品名称: Rottlerin
      CAS No.: 82-08-6
      Chemical Name: (2E)-1-[6-[(3-acetyl-2,4,6-trihydroxy-5-methylphenyl)methyl]-5,7-dihydroxy-2,2-dimethyl-2H-1-benzopyran-8-yl]-3-phenyl-2-propen-1-one
      Synonyms:Mallotoxin; NSC 56346; NSC 94525
      分子量:516.54
      分子式:C₃₀H₂₈O₈
      SMILES:O=C(C1=C2C(C=CC(C)(C)O2)=C(O)C(CC3=C(O)C(C)=C(O)C(C(C)=O)=C3O)=C1O)/C=C/C4=CC=CC=C4
      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: Rottlerin 是可从Mallotus Philippinensis中的到的一种天然产物, 是 PKC 的一个特异性抑制剂,其对PKCδ的IC50值为 3-6 μM, PKCα,β,γ 的为 30-42 μM,PKCε,η,ζ 为 80-100 μM。Rottlerin 可作为线粒体直接解偶联剂,通过编写那个mTOR1上游的信号级联刺激自噬。Rottlerin 通过活化caspase 3诱导细胞凋亡。
      IC50和靶点: [{name:"PKCδ:3 μM (IC50, Porcine spleen)"},{name: "PKCα:30 μM (IC50, baculovirus-infected Sf9 insect cells)"},{name: "PKCγ:40 μM (IC50, baculovirus-infected Sf9 insect cells)"},{name: "PKCβ:42 μM (IC50, baculovirus-infected Sf9 insect cells)"},{name: "PKCη:82 μM (IC50, baculovirus-infected Sf9 insect cells)"},{name: "PKCζ:100 μM (IC50, baculovirus-infected Sf9 insect cells)"},{name: "PKCε:100 μM (IC50, baculovirus-infected Sf9 insect cells)"},{name: "CaM kinase III:5.3 μM (IC50, EF-2 kinase activity in cytosol of murine pancreas)"},{name: "CKII:30 μM (IC50, holoenzyme expressed in E.coli)"},{name: "PKA:78 μM (IC50, catalytic subunit from porcine heart)'}, 'HIV-1']
      In Vitro:
      In Vivo:
      Clinical Trial:
      Solvent & Solubility:
    • McGovern, S.L., and Shoichet, B.K.Kinase inhibitors: Not just for kinases anymoreJ. Med. Chem.46(8),1478-1483(2003)

      Davies, S.P., Reddy, H., Caivano, M., et al.Specificity and mechanism of action of some commonly used protein kinase inhibitorsBiochem. J.351(1),95-105(2000)

      Balgi, A.D., Fonseca, B.D., Donohue, E., et al.Screen for chemical modulators of autophagy reveals novel therapeutic inhibitors of mTORC1 signalingPLoS One4(9),e7124(2009)

      Zhang, D., Anantharam, V., Kanthasamy, A., et al.Neuroprotective effect of protein kinase Cδ inhibitor rottlerin in cell culture and animal models of Parkinson's diseaseJ. Pharmacol. Exp. Ther.322(3),913-922(2007)

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