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> 产品中心 > 抑制剂 & 激动剂 > MAPK/ERK Pathway > MAPKAPK2 (MK2)

MK-2 Inhibitor III

Cat. No.:YN350083

  • CAS No. :1186648-22-5

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    • 参考文献
    • 产品名称: MK-2 Inhibitor III
      CAS No.: 1186648-22-5
      Chemical Name: 1,5,6,7-tetrahydro-2-[2-(3-quinolinyl)-4-pyridinyl]-4H-pyrrolo[3,2-c]pyridin-4-one, monohydrate
      Synonyms:MK-2 Inhibitor III
      分子量:358.39
      分子式:C₂₁H₁₈N₄O₂
      SMILES:O=C1C2=C(NC(C3=CC(C4=CC5=CC=CC=C5N=C4)=NC=C3)=C2)CCN1.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.
      Select Batch:
      Purity: 98%
    • 产品描述: MK-2 Inhibitor III (compound 16) 是一种具有口服活性的,选择性的,ATP 竞争性的MAPKAP-K2 (MK-2)抑制剂,IC50值为 0.85 nM,MK-2 Inhibitor III 对 MK-3 (IC50=0.21 μM), MK-5 (IC50=0.081 μM), ERK2 (IC50=3.44 μM), MNK1(IC50=5.7 μM) 以及 CDK2, JNK2, IKK2, MSK1, and MSK2 也具有选择性。
      IC50和靶点:
      In Vitro:
      In Vivo:
      Clinical Trial:
      Solvent & Solubility:
    • Huang, X., Shipps, G.W., Jr., Cheng, C.C., et al.Discovery and hit-to-lead optimization of non-ATP competitive MK2 (MAPKAPK2) inhibitorsACS Med. Chem. Lett.2(8),632-637(2011)

      Wang, X., Khaleque, M.A., Zhao, M.J., et al.Phosphorylation of HSF1 by MAPK-activated protein kinase 2 on serine 121, inhibits transcriptional activity and promotes HSP90 bindingJ. Biol. Chem.281(2),782-791(2006)

      Werz, O., Szellas, D., Steinhilber, D., et al.Arachidonic acid promotes phosphorylation of 5-lipoxygenase at Ser-271 by MAPK-activated protein kinase 2 (MK2)J. Biol. Chem.277(17),14793-14800(2002)

      Anderson, D.R., Meyers, M.J., Vernier, W.F., et al.Pyrrolopyridine inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2)J. Med. Chem.50(11),2647-2654(2007)

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