SB 525334
Chemical Name: 6-[2-(1,1-Dimethylethyl)-5-(6-methyl-2-pyridinyl)-1H-imidazol-4-yl]quinoxaline
Purity: ≥97%
Biological Activity
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.Technical Data
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.
Additional Information
Background References
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COL11A1 promotes tumor progression and predicts poor clinical outcome in ovarian cancer.
Wu Y, Chang T, Huang Y, Huang H, Chou C
Oncogene, 2014;33(26):3432-40. -
Progenitor-like traits contribute to patient survival and prognosis in oligodendroglial tumors.
Clin. Cancer Res., 2012;18(15):4122-35. -
R-Spondin1/LGR5 Activates TGF? Signaling and Suppresses Colon Cancer Metastasis
X Zhou, L Geng, D Wang, H Yi, G Talmon, J Wang
Cancer Res., 2017;0(0):. -
MicroRNA-214 antagonism protects against renal fibrosis.
Denby L, Ramdas V, Lu R, Conway B, Grant J, Dickinson B, Aurora A, McClure J, Kipgen D, Delles C, van Rooij E, Baker A
J Am Soc Nephrol, 2014;25(1):65-80. -
Inhibition of gene markers of fibrosis with a novel inhibitor of transforming growth factor-β type I receptor kinase in puromycin-induced nephritis.
Grygielko et al.
J.Pharmacol.Exp.Ther., 2005;313:943 -
Inhibition of AVNreceptor-like kinase 5 attenuates bleomycin-induced pulmonary fibrosis
Higashiyama et al.
Exp.Mol.Pathol., 2007;83:39 -
Tumor-specific efficacy of transforming growth factor-βRI inhibition in eker rats.
Laping et al.
Clin.Cancer Res., 2007;13:3087
Product Datasheets
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Citations for SB 525334
The citations listed below are publications that use Tocris products. Selected citations for SB 525334 include:
7 Citations: Showing 1 - 7
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Increased transforming growth factor beta (TGF-β) and pSMAD3 signaling in a Murine Model for Contrast Induced Kidney Injury.
Authors: Kilari Et al.
Sci Rep 2018;8:6630
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RECK-Mediated β1-Integrin Regulation by TGF-β1 Is Critical for Wound Contraction in Mice.
Authors: Gutiérrez Et al.
Lab Chip 2015;10:e0135005
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An Inducible TGF-β2-TGFβR Pathway Modulates the Sensitivity of HNSCC Cells to Tyrosine Kinase Inhibitors Targeting Dominant Receptor Tyrosine Kinases.
Authors: Kleczko Et al.
PLoS One 2015;10:e0123600
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MicroRNA-214 antagonism protects against renal fibrosis.
Authors: Denby Et al.
J Am Soc Nephrol 2014;25:65
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Epithelial-mesenchymal transition confers resistance to selective FGFR inhibitors in SNU-16 gastric cancer cells.
Authors: Grygielewicz Et al.
Gastric Cancer 2014;
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Flow-based pipeline for systematic modulation and analysis of 3D tumor microenvironments.
Authors: Li Et al.
Sci Rep 2013;13:1969
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Progenitor-like traits contribute to patient survival and prognosis in oligodendroglial tumors.
Authors: Ng Et al.
Clin Cancer Res 2012;18:4122
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