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LY364947 is a **selective small-molecule inhibitor** of the **transforming growth factor-beta type I receptor** (TGF-βRI, also known as ALK-5), acting as an ATP-competitive kinase inhibitor. It is used primarily as a research tool for dissecting TGF-β/SMAD signaling and has demonstrated efficacy in blocking phospho-SMAD2 and SMAD3 mediated signaling. LY364947 inhibits TGF-β–dependent cellular responses such as epithelial-mesenchymal transition (EMT), cell motility, and tumor invasion or progression in diverse preclinical cancer models, and has been studied in vitro and in vivo in the context of cancer and fibrosis. Its molecular formula is C17H12N4, with a molecular weight of 272.3, and the CAS number is 396129-53-6[1][3][5][6][7][9].
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