ML-228

ML-228 is an activator of the Hypoxia Inducible Factor (HIF) signaling pathway, as demonstrated by HIF response element (HRE) reporter assay (EC50 = 1.2 µM), HIF-1α nuclear translocation assay (EC50 = 1.3 µM), and increased VEGF expression (EC50 = 1.6 µM). Its activity in the HRE assay is blocked by excess iron, suggesting that ML-228 can chelate iron. ML-228 also significantly inhibits ligand binding to several channels, receptors, and transporters, including ERG potassium channel, 5-HT2B and A3 adenosine receptors, and dopamine transporter.