TB-500 exerts its effects primarily through promotion of actin polymerisation and cell migration. It upregulates the expression of beta-4 thymosin, which facilitates endothelial and muscle satellite cell movement to injury sites. Unlike BPC-157, TB-500 appears to act via a more systemic mechanism rather than locally at the administration site.

Tα1 modulates both innate and adaptive immune responses by stimulating the differentiation and maturation of T-cells, dendritic cells, and natural killer cells. It upregulates MHC class I and II expression, enhancing antigen presentation. It also promotes the production of key cytokines including interferon-γ and interleukin-2, which are central to immune surveillance.