SB 525334

Catalog # Availability Size / Price Qty
3211/10
3211/50
SB 525334 | CAS No. 356559-20-1 | TGF-beta Receptor Inhibitors
1 Image
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%

Product Details
Citations (7)
Supplemental Products
Reviews

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

M.Wt:
343.42
Formula:
C21H21N5
Solubility:
Soluble to 100 mM in DMSO
Purity:
≥97%
Storage:
Store at -20°C
CAS No:
356559-20-1

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

Licensing Caveats:
Sold with the permission of GlaxoSmithKline

Background References

  1. 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.
  2. Progenitor-like traits contribute to patient survival and prognosis in oligodendroglial tumors.

    Clin. Cancer Res., 2012;18(15):4122-35.
  3. 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):.
  4. 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.
  5. 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
  6. Inhibition of AVNreceptor-like kinase 5 attenuates bleomycin-induced pulmonary fibrosis
    Higashiyama et al.
    Exp.Mol.Pathol., 2007;83:39
  7. Tumor-specific efficacy of transforming growth factor-βRI inhibition in eker rats.
    Laping et al.
    Clin.Cancer Res., 2007;13:3087

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Citations for SB 525334

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