Tubulysin F is primarily recognized for its potent antitumor properties, making it a significant compound in cancer research. It functions by disrupting microtubule dynamics, which are crucial for cell division, thereby inhibiting the proliferation of cancer cells. Due to its high cytotoxicity, it is often explored in the development of targeted cancer therapies, particularly in drug conjugates where it is attached to antibodies or other targeting agents to deliver it directly to tumor cells while minimizing damage to healthy tissues. Its application is also being studied in the context of overcoming drug resistance in certain types of cancers, offering a potential avenue for more effective treatments.