Catalog Number: 3211
Chemical Name: 6-[2-(1,1-Dimethylethyl)-5-(6-methyl-2-pyridinyl)-1H-imidazol-4-yl]quinoxaline
Biological Activity
Selective inhibitor of transforming growth factor-β receptor I (ALK5, TGF-βRI) (IC50 = 14.3 nM). Inhibits TGF-β1-induced smad2/3 nuclear localization and TGF-βRI-induced mRNA expression in kidney cells. Attenuates bleomycin-induced pulmonary fibrosis.
Technical Data
  • M.Wt:
    343.42
  • Formula:
    C21H21N5
  • Solubility:
    Soluble to 100 mM in DMSO and to 100 mM in 1eq. HCl
  • Purity:
    >97%
  • Storage:
    Store at -20°C
  • CAS No:
    356559-20-1
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Additional Information
Licensing Caveats:
Sold with the permission of GlaxoSmithKline
Background References
  1. Inhibition of gene markers of fibrosis with a novel inhibitor of transforming growth factor-β type I receptor kinase in puromycin-induced nephritis.
    Grygielko et al.
    J.Pharmacol.Exp.Ther., 2005;313:943
  2. Inhibition of activin receptor-like kinase 5 attenuates bleomycin-induced pulmonary fibrosis
    Higashiyama et al.
    Exp.Mol.Pathol., 2007;83:39
  3. Tumor-specific efficacy of transforming growth factor-βRI inhibition in eker rats.
    Laping et al.
    Clin.Cancer Res., 2007;13:3087
Citations:

The citations listed below are publications that use Tocris products. Selected citations for SB 525334 include:

5 Citations: Showing 1 - 5
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  1. RECK-Mediated β1-Integrin Regulation by TGF-β1 Is Critical for Wound Contraction in Mice.
    Authors: Gutiérrez Et al.
    Lab Chip 2015;10:e0135005
  2. An Inducible TGF-β2-TGFβR Pathway Modulates the Sensitivity of HNSCC Cells to Tyrosine Kinase Inhibitors Targeting Dominant Receptor Tyrosine Kinases.
    Authors: Kleczko Et al.
    PLoS One 2015;10:e0123600
  3. Epithelial-mesenchymal transition confers resistance to selective FGFR inhibitors in SNU-16 gastric cancer cells.
    Authors: Grygielewicz Et al.
    Gastric Cancer 2014;
  4. Flow-based pipeline for systematic modulation and analysis of 3D tumor microenvironments.
    Authors: Li Et al.
    Sci Rep 2013;13:1969
  5. Progenitor-like traits contribute to patient survival and prognosis in oligodendroglial tumors.
    Authors: Ng Et al.
    Clin Cancer Res 2012;18:4122

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