Angiogenesis inhibition by the maleimide-based small molecule GNX-686

► We examined maleimide-based small molecule GNX-686 as anti-angiogenic agent in vitro and in vivo. ► GNX-686 significantly inhibits the tube formation of HUVEC at 4 μM. ► In the CAM model, GNX-686 inhibits the developmental angiogenesis as effectively as bevacizumab. ► GNX-686 reduces retinal microvasculature in the mouse ROP model.