515880-75-8

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).

DMH 4 is a selective VEGFR-2 inhibitor. DMH 4 displays antiangiogenic activity in vitro and in vivo.

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