**Background**
Vascular endothelial growth factor receptor 2 (VEGFR2) is a critical tyrosine kinase receptor located on the surface of endothelial cells. It plays a pivotal role in mediating the effects of VEGF, which is essential for angiogenesis, vasculogenesis, and vascular permeability. Overexpression or overactivation of the VEGFR2 signaling pathway is frequently associated with tumor growth and metastasis, as tumors rely on the formation of new blood vessels to supply oxygen and nutrients. Consequently, the development of potent and selective VEGFR2 inhibitors has become a primary focus in cancer therapy to inhibit tumor angiogenesis. In this context, we will introduce a selective VEGFR2 inhibitor – DMH4.
**Definition**
DMH4 is a potent and selective inhibitor of VEGFR2 with an IC50 value of 0.16 μM.
**In Vitro and In Vivo Studies**
Regarding the DMH4 description, this compound is a dorsomorphin analogue developed to improve selectivity toward specific kinase targets. According to the DMH4 technical information, it possesses a molecular weight of 400.47 and a chemical formula of C24H24N4O2. In studies evaluating DMH4 biological activity, researchers conducted structure-activity relationship analyses to identify analogues that could selectively inhibit VEGF and BMP signaling. DMH4 In Vitro assays demonstrated its high potency against VEGFR2, effectively blocking the downstream signaling pathways required for endothelial cell proliferation and migration. Furthermore, DMH4 In Vivo studies were utilized to assess the efficacy of these analogues in inhibiting angiogenesis and tumor growth in animal models, confirming that selective inhibition of VEGFR2 can significantly suppress the vascularization of tumors. In conclusion, DMH4 is a potent and selective VEGFR2 inhibitor that serves as a valuable tool for studying angiogenesis and developing anti-cancer therapeutic strategies.
Keywords
DMH4, 515880-75-8, DMH 4, DMH-4, VEGFR, Vascular endothelial growth factor receptor, Inhibitor, inhibitor, inhibit
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