DMH4 is an inhibitor of VEGF receptor 2 (VEGFR2; IC50 = 0.16 μM in a cell-free assay) and a derivative of dorsomorphin . It selectively inhibits VEGFR2 over activin receptor-like kinase 2 (ALK2), ALK5, and AMPK (IC50s = 3.5, >30, and 8 μM, respectively, in a cell-free assay). DMH4 inhibits growth of H460 and A549 human lung cancer cells (GI50s = 13.3 and 2.8 μM, respectively) and reduces VEGF-induced tubule formation in human umbilical vein endothelial cells (HUVECs; IC50 = 1 μM).
용도
DMH 4 is a selective VEGFR-2 inhibitor. DMH 4 displays antiangiogenic activity in vitro and in vivo.