NAMPT Degrader

PROTAC NAMPT Degrader-30 is a fluorescent PROTAC, which efficiently degrades NAMPT with an IC₅₀ of 41.9 nM. PROTAC NAMPT Degrader-30 binds to NAMPT and VHL to form a ternary complex and subsequently induced NAMPT degradation via ubiquitin-proteasome system (UPS). PROTAC NAMPT Degrader-30 leads to significant reduction of NAD⁺ and exerts potent antitumor activities.

PROTAC NAMPT Degrader-1 is a potent PROTAC targeting NAMPT with aDC₅₀ value of 217 nM. PROTAC NAMPT Degrader-1 has anti-proliferative activity with an IC₅₀ value of 0.12μM against A2780 cells. (Structure Note: PINK, NAMPT activator (HY-163445); Blue, VHL ligand (HY-163440); Black, linker).

PROTAC NAMPT Degrader-28 is a NAMPT PROTAC degrader with DC₅₀ values of 45 nM and 55 nM in MCF7 and 4T1cl5 cells, respectively. PROTAC NAMPT Degrader-28 retains nicotinamide phosphoribosyltransferase inhibitory activity and does not induce degradation of this enzyme. PROTAC NAMPT Degrader-28 can be used in breast cancer-related research.

NAMPT degrader-3 (compound C5) is a NAMPT degrader, depending on VHL- and proteasome manner. NAMPT degrader-3 displays cytotoxicity and inhibits A2780 cells proliferation.