LY-364947

LY-364947 is a chemical compound that acts as a selective inhibitor of the transforming growth factor-beta (TGF-β) receptor. It is primarily used in research settings to study the role of TGF-β signaling in various biological processes and diseases.

Chemical Properties

LY-364947 is a small molecule with the chemical formula C₂₂H₂₁N₅O₂. It is known for its ability to selectively inhibit the kinase activity of the TGF-β type I receptor, also known as ALK5 (activin receptor-like kinase 5).

Mechanism of Action

LY-364947 functions by binding to the ATP-binding site of the TGF-β type I receptor, thereby preventing the phosphorylation and activation of downstream signaling molecules such as SMAD2 and SMAD3. This inhibition blocks the TGF-β signaling pathway, which is involved in the regulation of cell growth, differentiation, and apoptosis.

Applications in Research

LY-364947 is widely used in preclinical studies to investigate the role of TGF-β signaling in various pathological conditions, including:

• Cancer: TGF-β signaling is known to play a dual role in cancer, acting as a tumor suppressor in early stages and promoting tumor progression in later stages. LY-364947 is used to study these mechanisms and to explore potential therapeutic interventions.
• Fibrosis: TGF-β is a key mediator of fibrosis in organs such as the liver, lungs, and kidneys. LY-364947 is used to investigate the potential of TGF-β inhibition as a treatment for fibrotic diseases.
• Cardiovascular diseases: The compound is used to study the role of TGF-β in cardiovascular remodeling and heart disease.

Safety and Toxicity

As LY-364947 is primarily used in laboratory research, detailed safety and toxicity profiles are not extensively documented for clinical use. However, researchers handling the compound should follow standard laboratory safety protocols.

Also see

• TGF-beta receptor
• SMAD proteins
• Kinase inhibitors
• Fibrosis
• Cancer research