Nampt-IN-5 is a potent and selective inhibitor of nicotinamide phosphoribosyltransferase (Nampt), an enzyme critical in the NAD+ salvage pathway. Its primary application lies in cancer research, where it is used to target tumor cells that rely heavily on Nampt for NAD+ production and energy metabolism. By inhibiting Nampt, Nampt-IN-5 induces NAD+ depletion, leading to reduced ATP levels and ultimately cancer cell death, especially in hematological malignancies and certain solid tumors.

It is also employed in studies exploring cellular metabolism, aging, and DNA repair mechanisms, as NAD+ plays a central role in these processes. Researchers use Nampt-IN-5 to modulate NAD+ levels and investigate downstream effects on sirtuin activity and mitochondrial function. Additionally, it has been utilized in combination therapies to enhance the efficacy of chemotherapeutic agents by weakening cancer cell metabolism and increasing susceptibility to apoptosis.