The conditions for optimal production of mycosporulone (1) are given. Its cytotoxic, antimicrobial, and antitumor activities are described. The biological activities of 1 were compared with those of known antibacterial, antifungal, and antitumor agents. The compound was particularly active against Pseudomonas aeruginosa and Staphylococcus aureus (resistant to penicillin). Compound 1 was not toxic to normal human cells (MRC(5)), although it exhibited cytotoxic activity against the human tumor cell lines MDA-MB 231 and PC(3) and the murine L-1210 leukemia cell line.