N,N'-dimethyl-N,N'-bis(mercaptoacetyl)hydrazine

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.

VEGFR2: 0.16 μM (IC₅₀)

[1] JIJUN HAO. In Vivo StructureActivity Relationship Study of Dorsomorphin Analogues Identifies Selective VEGF and BMP Inhibitors[J]. ACS Chemical Biology, 2009, 5 2: 245-253. DOI: 10.1021/cb9002865
[2] HAO LI . DMH4, a VEGFR2 inhibitor, effectively suppresses growth and invasion of lung cancer cells[J]. Journal of applied biomedicine, 2018, 16 1: Pages 46-50. DOI: 10.1016/j.jab.2017.10.006