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 (5)
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
1eq. HCl 34.34 100
DMSO 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.

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

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

Product Datasheets

Certificate of Analysis / Product Datasheet
Select another batch:
Safety Datasheet

References

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


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: 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

5 Citations for SB 525334

Citations are publications that use Tocris products. Selected citations for SB 525334 include:

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

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


Do you know of a great paper that uses SB 525334 from Tocris? If so please let us know.

Commented out for usability testing

Reviews

TODO: Add Reviews

Literature in this Area

Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Immunology

Immunology Product Listing

A collection of over 190 products for immunology research, the guide includes research tools for the study of:

  • Chemokine and Cytokine Signaling
  • Chemotaxis
  • Complement System
  • Immune Cell Signaling
  • Inflammation
Kinases

Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

  • Receptor Tyrosine Kinases
  • Protein Kinases A, C, D and G
  • PI-3 Kinase, Akt and mTOR
  • MAPK Signaling
  • Receptor Serine/Threonine Kinases
Stem Cells

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.

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.

Protocols

TODO: Add Protocols