The invention discloses a small molecule compound combination and a method for preparing vascular endothelial cells by using the small molecule compound combination to induce differentiated cells. According to the method, differentiated cells are subjected to targeted induction so as to finally obtain vascular endothelial cells, wherein the targeted induction comprises: inhibiting the activity oflysine deacetylase activity, inhibiting the signaling pathway of TGF-beta, inhibiting the activity of DNA methyltransferase (DNMT), activating the signaling pathway of WNT/beta-catenin, and activatingthe signaling pathway of cAMP. According to the present invention, through the induction with the small molecule compound combination, the differentiated cells can be transdifferentiated into the vascular endothelial cells, each step can be subjected to precise quality control, and the standardized operation and the large-scale production can be conveniently achieved; and the donor source of themethod is wide, the patient himself can be served as the donor, and the vascular endothelial cells required by basic research, clinical treatment or tissue engineering production can be obtained within a short time.