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SB-525334

Chemical Structure : SB-525334

CAS No.: 356559-20-1

SB-525334 (SB 525334, SB525334)

Catalog No.: PC-42858Not For Human Use, Lab Use Only.

SB-525334 is a potent and selective inhibitor of TGF-β1 receptor (ALK5) inhibitor with IC50 of 14,5 nM, 4-fold less potent against ALK4 and inactive for ALK2, ALK3, and ALK6 (IC50>10 uM).

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

SB-525334 is a potent and selective inhibitor of TGF-β1 receptor (ALK5) inhibitor with IC50 of 14,5 nM, 4-fold less potent against ALK4 and inactive for ALK2, ALK3, and ALK6 (IC50>10 uM).
SB 525334 blocks TGFβ1-induced phosphorylation and nuclear translocation of Smad2/3 in renal proximal tubule cells and inhibits TGFβ1-induced increases in PAI-1 and procollagen α1 mRNA expression in A498 renal epithelial carcinoma cells at 1 uM.
SB 525334 significantly inhibits PAN-induced proteinuria in rat model of nephritis-induced renal fibrosis.

Physicochemical Properties

M.Wt 343.4249
Formula C21H21N5
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: ≥ 46 mg/mL

Chemical Name/SMILES

Quinoxaline, 6-[2-(1,1-dimethylethyl)-5-(6-methyl-2-pyridinyl)-1H-imidazol-4-yl]-

References

1. Grygielko ET, et al. J Pharmacol Exp Ther. 2005 Jun;313(3):943-51.

2. Laping NJ, et al. Clin Cancer Res. 2007 May 15;13(10):3087-99.

3. Thomas M, et al. Am J Pathol. 2009 Feb;174(2):380-9.

4. Kim YJ, et al. Anticancer Res. 2012 Mar;32(3):799-806.

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