SB 525334

Pricing Availability Delivery Time Qty
Cat.No. 3211 - SB 525334 | C21H21N5 | CAS No. 356559-20-1
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)
Datasheet
Citations (6)
Reviews
Literature
Pathways

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

Compound Libraries

SB 525334 is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox I. Find out more about compound libraries available from Tocris.

Technical Data

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 34.34 100
1eq. HCl 34.34 100

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

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

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 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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View Related Products by Product Action

View all TGF-β Receptor Inhibitors

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

6 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

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

Denby et al (2014) MicroRNA-214 antagonism protects against renal fibrosis. J Am Soc Nephrol 25 65 PMID: 24158985

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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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.


Cancer

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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.

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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

TGF-β

TGF-β Signaling Pathway

The TGF-β signaling pathway is involved in the regulation of growth and proliferation of cells along with migration, differentiation and apoptosis.