A939572

• GMP format available

A939572 is a potent and orally bioavailable inhibitor of stearoyl-CoA desaturase 1 (SCD1), with IC50 values of <4 nM for mouse SCD1 and 37 nM for human SCD1.

Key features and applications include:

• High Selectivity: Specifically inhibits SCD1 with minimal off-target effects.
• Potency: Demonstrates strong inhibitory effects with low IC50 values.
• Inhibit Lipid Metabolism: Blocks the biosynthesis of monounsaturated fatty acids by inhibiting SCD1.
• Induce Cell Death: Promotes apoptosis in human pluripotent stem cells (hPSCs) and inhibits the proliferation of non-small cell lung carcinoma cells.
• Reduce Tumor Growth: Effective in various cancer models, both alone and in combination with other chemotherapeutics.

Relevant disease states include:

• Cancer: Active in models of clear cell renal cell carcinoma, bladder cancer, and non-small cell lung cancer.
• Obesity and Diabetes: SCD1 is a target for the treatment of obesity and diabetes due to its role in lipid metabolism.
• Cardiovascular Diseases: Potentially beneficial in reducing lipid-related cardiovascular risks.