NAMPT Degrader

PROTAC NAMPT Degrader-30 is a PROTAC degrader targeting nicotinamide phosphoribosyltransferase (NAMPT), with a DC₅₀ of 8.4 nM in A2780 cells. PROTAC NAMPT Degrader-30 binds to the VHL E3 ligase and forms a ternary complex with NAMPT, which induces ubiquitination and subsequent proteasomal degradation of NAMPT, thereby inhibiting the enzymatic activity of NAMPT. PROTAC NAMPT Degrader-30 reduces intracellular NAD⁺ levels and suppresses tumor cell proliferation. PROTAC NAMPT Degrader-30 exhibits a fluorescence turn-on response to the NAMPT protein, enabling real-time visualization of the NAMPT degradation process in living cells. PROTAC NAMPT Degrader-30 is applicable for research on ovarian cancer.

LYP-8 is an intracellular nicotinamide phosphoribosyltransferase (iNAMPT) PROTAC degrader with an IC₅₀ of 0.76 μM. LYP-8 recruits VHL E3 ligase to induce iNAMPT polyubiquitination and proteasome-dependent degradation, and inhibits iNAMPT enzymatic activity. LYP-8 reduces eNAMPT levels by degrading iNAMPT to decrease eNAMPT secretion. LYP-8 reduces intracellular NAD⁺ levels in cancer cells and proinflammatory cytokine levels (IL-6, TNF-α) in tumor tissue and serum. LYP-8 can be used for the research of colon cancer.

PROTAC NAMPT Degrader-31 is a PROTAC degrader that targets and degrades NAMPT by recruiting cereblon. It exhibits DC₅₀ values of 9.31 nM and 12.54 nM against NAMPT in MDA-MB-231 and 4T1 cells, respectively, and an IC₅₀ value of 15.05 nM for NAMPT enzymatic activity. PROTAC NAMPT Degrader-31 induces NAMPT degradation via the ubiquitin-proteasome system, inhibits NAMPT enzymatic activity, and reduces NAD⁺ levels through the NAD⁺ salvage pathway. It can be used in research related to triple-negative breast cancer.

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.

PROTEC NAMPT Degrader-1 is a NAMPT PROTEC degrader. PROTEC NAMPT Degrader-1 binds to NAMPT via non-covalent interactions and degrades this protein through a proximity-induced radical oxidation mechanism mediated by cyclopropane radical clock, independent of proteasomal or lysosomal pathways. PROTEC NAMPT Degrader-1 exhibits anticancer activity against ovarian cancer. It can be used in relevant studies on ovarian cancer (Pink: NAMPT ligand: (HY-188123); Linker: (HY-188124)).

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.