incb-000928 fumarate, nbu-928 fumarate

Zilurgisertib fumarate (INB-000928 fumarate) is a potent and selective inhibitor of Activin Receptor-Like Kinase 2 (ALK2/ACVR1). It significantly inhibits ALK2 kinase activity (IC50 = 15 nM) and downregulates BMP-6-induced SMAD1/5 phosphorylation (IC50 = 63 nM). By blocking ALK2-mediated signaling, Zilurgisertib suppresses the production of hepcidin in hepatocytes (IC50 = 20 nM), thereby modulating iron metabolism. In preclinical studies, Zilurgisertib demonstrates the potential to improve anemia in cancer-induced models by effectively increasing hemoglobin levels.

Zilurgisertib (INCB-000928) is a selective and potent ALK 2 inhibitor for the study of cancer and MF anemia.