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

PF-3644022

Cat. No.:YN350049

  • CAS No. :1276121-88-0

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    • 参考文献
    • 产品名称: PF-3644022
      CAS No.: 1276121-88-0
      Chemical Name: (10R)-9,10,11,12-tetrahydro-10-methyl-3-(6-methyl-3-pyridinyl)-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one
      Synonyms:PF 3644022;PF3644022
      分子量:374.46
      分子式:C₂₁H₁₈N₄OS
      SMILES:O=C1C2=C(NC[C@@H](C)N1)C3=C(C=CC4=NC(C5=CN=C(C)C=C5)=CC=C34)S2
      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: PF-3644022 是一种有效的,选择性的,口服活性的,具有 ATP 竞争性的MAPKAPK2 (MK2)抑制剂,IC50为 5.2 nM,Ki为 3 nM。PF-3644022 还抑制 MK3 和 p38 调节/激活激酶 (PRAK),IC50分别为 53 nM 和 5.0 nM。PF-3644022 有效抑制 TNFα 的产生并具有抗炎作用。
      IC50和靶点:
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      In Vivo:
      Clinical Trial:
      Solvent & Solubility:
    • Mourey, R.J., Burnette, B.L., Brustkern, S.J., et al.A benzothiophene inhibitor of mitogen-activated protein kinase-activated protein kinase 2 inhibits tumor necrosis factor α production and has oral anti-inflammatory efficacy in acute and chronic models of inflammationJ. Pharmacol. Exp. Ther.333(3),797-807(2010)

      Yu, L., Song, H., Fang, X., et al.Role of MK2 signaling pathway mediating microglia/macrophages polarization in chronic compression injury of cervical spinal cordAnn. Palliat. Med.10(2),1304-1312(2021)

      Berggren, K.L., Cruz, S.R., Hixon, M.D., et al.MAPKAPK2 (MK2) inhibition mediates radiation-induced inflammatory cytokine production and tumor growth in head and neck squamous cell carcinomaOncogene38(48),7329-7341(2019)

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