SB 525334

Cat. No. 3211

SB 525334 C21H21N5 [356559-20-1]

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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

Soluble to 100 mM in DMSO and to 100 mM in 1eq. HCl
>97 %
Store at -20°C

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.

Certificate of Analysis / Safety Data Sheet

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Safety Data Sheet: View Safety Data Sheet

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.

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.

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

Citations are publications that use Tocris products. Selected citations for SB 525334 include:

Gutiérrez et al (2015) RECK-Mediated β1-Integrin Regulation by TGF-β1 Is Critical for Wound Contraction in Mice. Lab Chip 10 e0135005. PMID: 26247610.

Kleczko et al (2015) An Inducible TGF-β2-TGFβR Pathway Modulates the Sensitivity of HNSCC Cells to Tyrosine Kinase Inhibitors Targeting Dominant Receptor Tyrosine Kinases. PLoS One 10 e0123600. PMID: 25946135.

Grygielewicz et al (2014) Epithelial-mesenchymal transition confers resistance to selective FGFR inhibitors in SNU-16 gastric cancer cells. Gastric Cancer. PMID: 25407459.

Li et al (2013) Flow-based pipeline for systematic modulation and analysis of 3D tumor microenvironments. Sci Rep 13 1969. PMID: 23563587.

Ng et al (2012) Progenitor-like traits contribute to patient survival and prognosis in oligodendroglial tumors. Clin Cancer Res 18 4122. PMID: 22675171.

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