It is known that bufalin targets SRC-1/3 for cancer treatment (Wang et al., 2014), while growing evidence suggests that bufalin could also target or downregulate many essential enzymes/proteins in cancer cells, including ATP1A1 (Lan et al., 2018), specific miRNA (Liu et al., 2017), AMPK/mTOR pathway (Shen et al., 2014), p-Akt (Wang et al., 2018b) and Met/PI3K/Akt pathway (Kang et al., 2013), MRP1 (Gu et al., 2014) etc., suggesting that it is a multi-targeting or multi-functional agent. Here, ATP1A1 is linked to cancer.