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.
Sold with the permission of GlaxoSmithKline
|Storage||Store at -20°C|
All Tocris products are intended for laboratory research use only.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 343.42. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.91 mL||14.56 mL||29.12 mL|
|5 mM||0.58 mL||2.91 mL||5.82 mL|
|10 mM||0.29 mL||1.46 mL||2.91 mL|
|50 mM||0.06 mL||0.29 mL||0.58 mL|
References are publications that support the products' biological activity.
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
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Keywords: SB 525334, supplier, Selective, inhibitors, inhibits, TGF-βRI, TGF-β, TGF-betaRI, TGFbRI, TGFbR1, tgf-b1Transforming, Growth, Factors, Beta, Receptors, TGF-beta, Receptor, Serine/Threonine, Kinases, RSTKs, SB525334, GlaxoSmithKline, GSK, TGF-beta, Receptors, TGF-beta, Receptors, Tocris Bioscience
5 Citations for SB 525334
Citations are publications that use Tocris products. Selected citations for SB 525334 include:
Li et al (2013) Flow-based pipeline for systematic modulation and analysis of 3D tumor microenvironments. Sci Rep 13 1969 PMID: 23563587
Grygielewicz et al (2014) Epithelial-mesenchymal transition confers resistance to selective FGFR inhibitors in SNU-16 gastric cancer cells. Gastric Cancer PMID: 25407459
Ng et al (2012) Progenitor-like traits contribute to patient survival and prognosis in oligodendroglial tumors. Clin Cancer Res 18 4122 PMID: 22675171
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
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
Do you know of a great paper that uses SB 525334 from Tocris? If so please let us know.
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