Tubulysin G is primarily investigated for its potent anticancer properties. It functions by disrupting microtubule dynamics, which are essential for cell division, making it highly effective in inhibiting the proliferation of cancer cells. Researchers are exploring its use in targeted cancer therapies, particularly in drug conjugates where it is attached to antibodies or other targeting molecules to deliver the compound directly to tumor cells, minimizing damage to healthy tissues. Its strong cytotoxic activity has shown promise in preclinical studies against various cancer types, including drug-resistant tumors. Additionally, Tubulysin G is being studied for its potential in combination therapies to enhance the efficacy of existing cancer treatments.