Dehydroaltenusin (38.0 μM; 6 hours) inhibits cell growth by blocking the S-phase of DNA replication. Dehydroaltenusin (38.0-44.4 μM; 24 hours) inhibits cell growth in a dose-dependent manner (LD50s: 38.0 to 44.4 μM). Dehydroaltenusin (75.0 μM; 24 hours) has a potent apoptotic effect on human cancer cells, DNA ladders can be detected after 12 h of incubation with dehydroaltenusin.

Dehydroaltenusin possesses anti-tumor activity against human adenocarcinoma tumors in vivo. Dehydroaltenusin (injection; 20 mg/kg; 2-day intervals; 12-39 days) shows suppressed tumor growth from 21 days.