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BIX02189

Cat. No.:YN350098

  • CAS No. :1265916-41-3

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    • 产品名称: BIX02189
      CAS No.: 1265916-41-3
      Chemical Name: (3Z)-3-[[[3-[(dimethylamino)methyl]phenyl]amino]phenylmethylene]-2,3-dihydro-N,N-dimethyl-2-oxo-1H-indole-6-carboxamide
      Synonyms:BIX 02189
      分子量:440.54
      分子式:C₂₇H₂₈N₄O₂
      SMILES:O=C(N(C)C)C1=CC(NC2=O)=C(/C2=C(C3=CC=CC=C3)/NC4=CC=CC(CN(C)C)=C4)C=C1.[(Z)]
      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: BIX02189 是一种有效的选择性MEK5抑制剂,IC50为 1.5 nM。BIX02189 也抑制ERK5活性,IC50为 59 nM。
      IC50和靶点: [{name:"MEK5:1.5 nM (IC50)"},{name: "ERK5:59 nM (IC50)"},{name: "CSF1R (FMS):46 nM (IC50)"},{name: "LCK:250 nM (IC50)"},{name: "JAK3:440 nM (IC50)"},{name: "TGFβR1:580 nM (IC50)"},{name: "RPS6KA6 (RSK4):990 nM (IC50)"},{name: "RPS6KA3 (RSK2):2.1 μM (IC50)"},{name: "FGFR1:1 μM (IC50)"},{name: "KIT:1.1 μM (IC50)"},{name: "ABL1:2.4 μM (IC50)"},{name: "MAPK14 (p38 alpha):3.7 μM (IC50)"},{name: "SRC:7.6 μM (IC50)"}]
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      In Vivo:
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    • Tatake, R.J., O'Neill, M.M., Kennedy, C.A., et al.Identification of pharmacological inhibitors of the MEK5/ERK5 pathwayBiochem. Biophys. Res. Commun.377(1),120-125(2008)

      Obara, Y., and Nakahata, N.The signaling pathway leading to extracellular signal-regulated kinase 5 (ERK5) activation via G-proteins and ERK5-dependent neurotrophic effectsMol. Pharmacol.77(1),10-16(2010)

      Wang, X., Pesakhov, S., Weng, A., et al.ERK 5/MAPK pathway has a major role in 1a,25-(OH)2 vitamin D3-induced terminal differentiation of myeloid leukemia cellsJ. Steroid Biochem. Mol. Biol.144(Pt. A),223-227(2014)

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