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Cat. No. Name Size Price Add Cart
KI3360SB 525334QuoteQuote

Chemical Characteristic

Product NameSB 525334
CAS No.356559-20-1
Molecular Weight 343.42
FormulaC21H21N5
Chemical Name6-[2-tert-butyl-5-(6-methylpyridin-2-yl)-1H-imidazol-4-yl]quinoxaline
Smilesn1ccnc2cc(ccc12)c1nc([nH]c1c1cccc(n1)C)C(C)(C)C
Chemical Structure

Biological activities

SB525334 is a potent and selective inhibitor of the transforming growth factor-β1 (TGF-β1) receptor (ALK5). The IC50 of SB525334 against ALK5 is 14.3 nM. SB525334 is less potent to inhibit ALK4 with an IC50 of 58.5 nM. SB525334 is inactive to inhibit ALK2, ALK3, and ALK6. In vitro, SB525334 (1 µM) blocks TGF-β1-induced phosphorylation and nuclear translocation of Smad2/3 in renal proximal tubule cells. SB525334 also inhibits the mRNA expression of plasminogen activator inhibitor-1 (PAI-1) and procollagen α1(I) induced by TGF-β1 in A498 renal epithelial carcinoma cells.[1] In the acute puromycin aminonucleoside (PAN) rat model of renal disease in vivo, orally administration of SB525334 (1, 3, or 10 mg/kg/day) dose-dependently decreases renal procollagen alpha1(I) and procollagen alpha1(III) mRNA, and also causes significant reduction in renal PAI-1 mRNA.[1] In mesenchymal (leiomyoma) tumors in Eker rats, SB525334 administration significantly decreases tumor incidence and multiplicity, and reduces the size of mesenchymal tumors. In epithelial (renal cell carcinoma) tumors in Eker rats, SB525334 administration also promotes the development of epithelial tumors.[2] In the Bleomycin (BLM)-induced pulmonary fibrosis model, SB525334 treatment attenuates R-Smads activation thereby attenuates pulmonary fibrosis.[3]

Protocols

In vivo, SB525334 is dissolved with 10% PEG 400, containing 0.75% DMSO and adjusted at pH 3 with HCl, at a volume of 1 mg/mL.[3]

References

[1] Grygielko ET, et al. Inhibition of gene markers of fibrosis with a novel inhibitor of transforming growth factor-beta type I receptor kinase in puromycin-induced nephritis. J Pharmacol Exp Ther. 2005, 313(3): 943-951.
[2] Laping NJ, et al. Tumor-specific efficacy of transforming growth factor-beta RI inhibition in Eker rats. Clin Cancer Res. 2007, 13(10): 3087-3099.
[3] Higashiyama H, et al. Inhibition of activin receptor-like kinase 5 attenuates bleomycin-induced pulmonary fibrosis. Exp Mol Pathol. 2007, 83(1): 39-46.

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