GGTI 2133 is primarily used in research settings to study the role of geranylgeranyltransferase I (GGTase I) in cellular processes. It is a potent inhibitor of GGTase I, an enzyme involved in the post-translational modification of proteins, particularly those in the Ras and Rho superfamilies. By inhibiting this enzyme, GGTI 2133 helps researchers understand the signaling pathways and mechanisms related to cell growth, differentiation, survival, and apoptosis.

It is particularly useful in cancer research, as it provides insights into how inhibiting protein prenylation (geranylgeranylation) can affect tumor progression, metastasis, invasion, and induction of apoptosis in cancer cells. Additionally, GGTI 2133 is employed in studies exploring inflammation, cardiovascular diseases, and neurological disorders such as Alzheimer's, where GGTase I plays a significant role in protein function and cellular degeneration.

Its application extends to drug development, where it serves as a tool to identify potential therapeutic targets for diseases linked to abnormal protein prenylation, aiding in the understanding of disease mechanisms and the development of new treatments.