GSK-503

GSK-503 is a potent EZH2 inhibitor with potential anticancer activity. Increased activity of the epigenetic modifier EZH2 has been associated with different cancers. In a melanoma mouse model, conditional Ezh2 ablation as much as treatment with the preclinical EZH2 inhibitor GSK503 stabilizes the disease through inhibition of growth and virtually abolishes metastases formation without affecting normal melanocyte biology.