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Biological Activity:
Potent inhibitor of TGF-β type I receptor superfamily activin-like kinase ALK5 with IC50 of 25 nM. A-77-01 is a close analogue of A-83-01 (Axon 1421) and has a very similar biological profile of A-83-01.
A-83-01 is found to decompose to A-77-01 under certain circumstances and A-77-01 is likely an active component or metabolite of its prodrug A-83-01.
References:
M Tojo et al. The ALK5 inhibitor A-83-01 inhibits smad signaling and epithelial-to-mesenchymal transition by transforming growth factor-β. Cancer. Sci. 2005, 96, 791-800. [online]
Chemical Name: 4-(3-(6-methylpyridin-2-yl)-1H-pyrazol-4-yl)quinoline
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