Nampt degrader-2, a fluorescent PROTAC, exhibits efficient degradation of NAMPT at an IC50 of 41.9 nM. It operates by binding to both NAMPT and VHL, initiating the formation of a ternary complex that triggers NAMPT degradation through the ubiquitin-proteasome system (UPS). This activity significantly lowers NAD+ levels and displays potent antitumor effects [1].

NAMPT:41.9 nM