2484876-99-3
Chemical Structure
LYP-8
- CAS 番号: 2484876-99-3
- Formula:C56H74N8O10S
- Molecular Weight:1051.30
InChIKey: USOZUDKPZDDZBP-BLKHOLARSA-N
SMILES: CC1=C(SC=N1)C2=CC=C(C=C2)[C@@H](NC([C@@H]3C[C@H](CN3C([C@H](C(C)(C)C)NC(COCCOCCOCCNC(C4=CC=C(C=C4)C(N5CCC(CC5)CCCCNC(/C=C/C6=CN=CC=C6)=O)=O)=O)=O)=O)O)=O)C
Biological Activity: 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[1].
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LYP-8 | 99.89% | 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. | ||||||||||||||||||||
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