In the present study, we demonstrated ZY0511 effectively inhibited hepatocellular carcinoma (HCC) cell proliferation by upregulating the expression of DNA damage‐inducible gene 45beta (GADD45B), a direct downstream target of lysine‐specific histone demethylase 1 (LSD1). The gene discussed is KDM1A; the disease is hepatocellular carcinoma.