Bufalin has been shown to inhibit SRC‐1 in cancer cells,43 and Wortmannin is an effective PI3K inhibitor.51 To explore whether SRC‐1 and PI3K were involved in the GPR30 regulation of mTORC2 signals, actin cytoskeleton remodeling, and synaptic proteins, we treated the mHippoE‐14 cells with G1, Bufalin, and Wortmannin separately or in combination. This evidence concerns the gene GPER1 and cancer.