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A8300 Case Study

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A8301

Description:
IC50: 18 nM for ALK5

GW788388 is a selective inhibitor of ALK5 and TGF-β

Progressive kidney fibrosis precedes end-stage renal failure in patients with diabetes mellitus. Elevated transforming growth factor-b (TGF-β) is considered to underlie disease progression via promoting extracellular matrix deposition as well as epithelial–mesenchymal transition. TGF-β signals through the TGF-β type I receptor also are named activin receptor-like kinase (ALK) 5.

In vitro: GW788388 inhibited both the TGF-β type I and type II receptor kinase activities, but not that of the related bone morphogenic protein type II receptor. In addition, GW788388 could blockTGF-β-induced Smad activation and target gene expression, while decrease epithelial–mesenchymal

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