PROTACs Degrader
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LYP-8
0 ImagesLYP-8 is an intracellular nicotinamide phosphoribosyltransferase (iNAMPT) inhibitor with an IC50 of 0.76 μM, a reducing agent, and a tumor growth inhibitor. 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.
