10058-F4 is a potent and selective c-Myc inhibitor, which markedly increases valproic acid-induced cell death in Jurkat and CCRF-CEM T-lymphoblastic leukemia cells. 10058-F4 inhibits proliferation, downregulates human telomerase reverse transcriptase and enhances chemosensitivity in human hepatocellular carcinoma cells. 10058-F4 induces cell-cycle arrest, apoptosis, and myeloid differentiation of human acute myeloid leukemia.