To explore the anti-chronic myelogenous leukemia (CML) activity of rocaglamide (RocA) caused by aerobic glycolysis and potent molecular mechanism,the proliferation of CML cell line K562 inhibited by RocA were determined.The MTT assay showed that RocA inhibited the proliferation of K562 in a time-and dose-dependent way.The IC50 of K562 treated with RocA for 3 days was 21.70±5.68 nmol/L.Flow cytometry analyzed that the proportion of cells of G2/M phase was significantly increased.The apoptotic cells was significantly increased.RocA decreased the glucose consumption,lactate acid production and the protein expression of hexokinase 2 (HK2),c-Myc,which take an important part in aerobic glycolysis.The propagation rate,lactate acid production and the c-Myc protein expressionof K562 cells cultured without glucose was significantly lower than that cultured with glucose.After treatment with RocA,the inhibition on K562 cells cultured without glucose was significantly decreased compared to K562 cells cultured with glucose.Taken together,we presumed that RocA inhibited the proliferation of CML cells via apoptosis induction and cycle arrest partly through c-Myc/HK2 mediated aerobic glycolysis suppression.