SB-525334 | ALK5 inhibitor
NMR (Conforms)
Available Options
| Size : | Price | Quantity | |
|---|---|---|---|
| 5 mg | $60.00 | ||
| 25 mg | $220.00 |
SB-525334 (356559-20-1) is a potent and selective inhibitor of the transforming growth factor beta 1 receptor, activin receptor-like kinase (ALK5) (IC50 = 14.3 nM) and ALK4, (IC50 = 58.5 nM) with no activity at ALK2, 3 and 6.1 Blocks fibrosis markers and renal injury in the puromycin-induced nephritis model.1 SB-525334 causes significant attenuation in Smad2/3 nuclear translocation, decrease in CTGF-expressing cells, myofibroblast proliferation and type 1 collagen deposition resulting in an overall attenuation in bleomycin-induced pulmonary fibrosis.2 Sensitizes drug-resistant pancreatic cancer cells to gemcitabine.3 Cell permeable and active in vivo.
References/Citations:
1) Grygielko et al. (2005), 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., 313 943
2) Higashiyama et al. (2007), Inhibition of activin receptor-like kinase 5 attenuates bleomycin-induced pulmonary fibrosis; Exp. Mol. Pathol., 83 39
3) Kim et al. (2012), Transforming growth factor beta receptor I inhibitor sensitizes drug-resistant pancreatic cancer cells to gemcitabine; Anticancer Res., 32 799
NMR (Conforms)
Safety Data Sheet:
Product Data Sheet:
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee
SB-525334 (356559-20-1) is a potent and selective inhibitor of the transforming growth factor beta 1 receptor, activin receptor-like kinase (ALK5) (IC50 = 14.3 nM) and ALK4, (IC50 = 58.5 nM) with no activity at ALK2, 3 and 6.1 Blocks fibrosis markers and renal injury in the puromycin-induced nephritis model.1 SB-525334 causes significant attenuation in Smad2/3 nuclear translocation, decrease in CTGF-expressing cells, myofibroblast proliferation and type 1 collagen deposition resulting in an overall attenuation in bleomycin-induced pulmonary fibrosis.2 Sensitizes drug-resistant pancreatic cancer cells to gemcitabine.3 Cell permeable and active in vivo.
References/Citations:
1) Grygielko et al. (2005), 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., 313 943
2) Higashiyama et al. (2007), Inhibition of activin receptor-like kinase 5 attenuates bleomycin-induced pulmonary fibrosis; Exp. Mol. Pathol., 83 39
3) Kim et al. (2012), Transforming growth factor beta receptor I inhibitor sensitizes drug-resistant pancreatic cancer cells to gemcitabine; Anticancer Res., 32 799
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