SB 525334

Pricing Availability   Qty
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 (7)
Reviews
Literature (3)
Pathways (1)

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.

Select a batch to recalculate based on the batch molecular weight:
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

Certificate of Analysis / Product Datasheet
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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.

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

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

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

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


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Reviews for SB 525334

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Literature in this Area

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Pathways for SB 525334

TGF-β Signaling Pathway

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.