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:
  • Formula:
  • Solubility:
    Soluble to 100 mM in DMSO and to 100 mM in 1eq. HCl
  • Purity:
  • Storage:
    Store at -20°C
  • CAS No:
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
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