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Submit ReviewSB 525334
Description: Selective inhibitor of TGF-βRI
Chemical Name: 6-[2-(1,1-Dimethylethyl)-5-(6-methyl-2-pyridinyl)-1H-imidazol-4-yl]quinoxaline
Purity: ≥97% (HPLC)
Biological Activity for SB 525334
SB 525334 is a 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
Compound Libraries for SB 525334
SB 525334 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.
Technical Data for SB 525334
| M. Wt | 343.42 |
| Formula | C21H21N5 |
| Storage | Store at -20°C |
| Purity | ≥97% (HPLC) |
| CAS Number | 356559-20-1 |
| PubChem ID | 9967941 |
| InChI Key | DKPQHFZUICCZHF-UHFFFAOYSA-N |
| Smiles | CC1=NC(C4=C(NC(C(C)(C)C)=N4)C2=CC=C(N=CC=N3)C3=C2)=CC=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for SB 525334
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 34.34 | 100 |
Preparing Stock Solutions for SB 525334
The following data is based on the product molecular weight 343.42. Batch specific molecular weights may vary from batch to batch due to the degree 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 |
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Product Datasheets for SB 525334
References for SB 525334
References are publications that support the biological activity of the product.
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 AVNreceptor-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 reference for SB 525334, please let us know.
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Keywords: SB 525334, 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, 3211, Tocris Bioscience
7 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
Ng et al (2012) Progenitor-like traits contribute to patient survival and prognosis in oligodendroglial tumors. Clin Cancer Res 18 4122 PMID: 22675171
Kilari et al (2018) Increased transforming growth factor beta (TGF-β) and pSMAD3 signaling in a Murine Model for Contrast Induced Kidney Injury. Sci Rep 8 6630 PMID: 29700311
Denby et al (2014) MicroRNA-214 antagonism protects against renal fibrosis. J Am Soc Nephrol 25 65 PMID: 24158985
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
Grygielewicz et al (2014) Epithelial-mesenchymal transition confers resistance to selective FGFR inhibitors in SNU-16 gastric cancer cells. Gastric Cancer PMID: 25407459
Do you know of a great paper that uses SB 525334 from Tocris? Please let us know.
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Stem Cell Research Product Guide
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Stem Cells Scientific Review
Written by Kirsty E. Clarke, Victoria B. Christie, Andy Whiting and Stefan A. Przyborski, this review provides an overview of the use of small molecules in the control of stem cell growth and differentiation. Key signaling pathways are highlighted, and the regulation of ES cell self-renewal and somatic cell reprogramming is discussed. Compounds available from Tocris are listed.
Stem Cells Poster
Written by Rebecca Quelch and Stefan Przyborski from Durham University (UK), this poster describes the isolation of pluripotent stem cells, their maintenance in culture, differentiation, and the generation and potential uses of organoids.
Pathways for SB 525334
