Drug intelligence / Profile preview

LY364947

Development stage
Preclinical
Lead developer
Eli Lilly
Modality
Small Molecules
Administration
Intraperitoneal (in Animal Models), Not For Clinical Human Use
01

Overview

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].

Other names
TbetaR-I InhibitorTransforming Growth Factor-beta Type I Receptor Kinase Inhibitor
02

Targets

PK (Pyruvate kinase)TGFBR1RK (Ribokinase)TGFBR2 (TGF-β receptor type 2)

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