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SB 525334

Cat. No. 3211

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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.

Licensing Information

Sold with the permission of GlaxoSmithKline

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.

Resources

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch

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Safety Data Sheet: View Safety Data Sheet

References

Grygielko et al (2005) Inhibition of gene markers of fibrosis with a novel inhibitor of transforming growth factor-β type I receptor kinase in puromycin-induced nephritis. J.Pharmacol.Exp.Ther. 313 943. PMID: 15769863.

Higashiyama et al (2007) Inhibition of activin receptor-like kinase 5 attenuates bleomycin-induced pulmonary fibrosis Exp.Mol.Pathol. 83 39. PMID: 17274978.

Laping et al (2007) Tumor-specific efficacy of transforming growth factor-βRI inhibition in eker rats. Clin.Cancer Res. 13 3087. PMID: 17505012.

If you know of a relevant citation for this product please let us know.

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