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Product Details

SB-525334 | ALK5 (TGFbeta R1) inhibitor

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 gemcitabine3. 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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Catalog#  10-2983

$60.00
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CAS:
356559-20-1
Catalog Number:
10-2983
Activity:
ALK5 (TGFβR1) inhibitor
Chemical Name:
6-[2-(1,1-Dimethylethyl)-5-(6-methyl-2-pyridinyl)-1H-imidazol-4-yl]quinoxaline
Molecular Weight:
343.42
Molecular Formula:
C21H21N5
Solubility:
Soluble in DMSO (up tp 30 mg/ml)
Physical Properties:
Yellow solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
-20°C (des.)
Stability:
Stable for 2 years as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

Focus BiomoleculesPlymouth Meeting, PA USA1-855-FOCUS21

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