Chemical Name: 6-[2-(1,1-Dimethylethyl)-5-(6-methyl-2-pyridinyl)-1H-imidazol-4-yl]quinoxaline
ALK5 (TGFbetaR1) inhibitor
Molekulargewicht:
343.42
Reinheit:
98% by HPLC NMR (Conforms)
Formulierung:
Yellow solid
CAS Nummer:
[356559-20-1]
Formel:
C21H21N5
Anwendungsbeschreibung:
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 61. Blocks fibrosis markers and renal injury in the puromycin-induced nephritis model1. It 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 fibrosis2. Sensitizes drug-resistant pancreatic cancer cells to gemcitabine3. Cell permeable and active in vivo.
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