NAMPT PROTAC A7 is a potent and selective intracellular nicotinamide phosphoribosyl transferase (iNAMPT) Degrader (PROTAC™;) (IC50 of 9.5 nM against the enzymatic activity of NAMPT). Comprises a potent NAMPT inhibitor joined by a linker to a ligand for Von Hippel-Lindau (VHL) protein. Proteomic analysis of global protein level changes confirms selectivity. NAMPT PROTAC A7 decreases iNAMPT level and the secretion of extracellular NAMPT (eNAMPT) in CT26 or MC38 cells. In CT26 tumor bearing BALB/c mice, the compound degrades tumoral NAMPT, and boosts antitumor immunity by inhibiting tumor infiltrating myeloid-derived suppressive cells.
PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.
Caractéristiques techniques
| Marque | Tocris Bioscience |
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| Réf. B-LABO | BL-RE-125976 |
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| Réf. fabricant | 30000028 |
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| Nom chimique ou matériau | (2S,4R)-1-((S)-18-(tert-Butyl)-1,16-dioxo-1-(4-((4-((4-(3-(pyridin-3-ylmethyl)thioureido)phenyl)sulfonyl)piperazin-1-yl)methyl)phenyl)-5,8,11,14-tetraoxa-2,17-diazanonadecan-19-oyl)-4-hydroxy-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-ca |
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| CAS | 2484876-94-8 |
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| Quantité | 5 mg |
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| Cible | Active Degraders |
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| Formule moléculaire | C<sub>58</sub>H<sub>76</sub>N<sub>10</sub>O<sub>11</sub>S<sub>3</sub> |
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| Pureté | 0.98 |
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