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-im idazol-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 localisation and TGF-β1-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:
>98 %
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 and MSDS.

Certificate of Analysis / MSDS

Certificate of Analysis: View current batch
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Material Safety Data Sheet: View current batch
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References

Grygielko et al (2005) Inhibition of gene markers of fibrosis with a novel inhibitor of transforming growth factor-b type I receptor kinase in puromycin-induced nephritis. J.Pharmacol.Exp.Ther. 313 943. Higashiyama et al (2007) Inhibition of activin receptor-like kinase 5 attenuates bleomycin-induced pulmonary fibrosis. Exp.Mol.Pathol. 83 39. Laping et al (2007) Tumor-specific efficacy of transforming growth factor-bRI inhibition in eker rats. Clin.Cancer Res. 13 3087.

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Keywords: SB 525334, Selective, inhibitors, TGF-βRI, TGF-β, TGF-betaRI, TGFbRI, TGFbR1, tgf-b1Transforming, Growth, Factor, Beta, Receptors, TGF-β, TGF-beta, Receptor, Serine/Threonine, Kinases, RSTKs, SB525334, GlaxoSmithKline

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