Application

A 83-01 has been used as an inhibitor of transforming growth factor β kinase type 1 receptor.

Biochem/physiol Actions

A 83-01 is a TGFβ kinase/activin receptor-like kinase (ALK 5) inhibitor (IC₅₀=12 nM) that prevents phosphorylation of Smad2/3 and inhibits growth induced by TGFβ. A 83-01 blocks phosphorylation of Smad2 and inhibits TGF-β-induced epithelial-to-mesenchymal transition. Also, A 83-01 inhibits the transcriptional activity induced by TGFβ type I receptor ALK-5, activin type IB receptor ALK-4 and nodal type I receptor ALK-7. A-83-01 induces an expansion of neonatal Nkx2.5-eGFP (+) cells.

Packaging

5, 25 mg in glass bottle