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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.
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
The following data is based on the product molecular weight 1185.49. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|0.2 mM||4.22 mL||21.09 mL||42.18 mL|
|1 mM||0.84 mL||4.22 mL||8.44 mL|
|2 mM||0.42 mL||2.11 mL||4.22 mL|
|10 mM||0.08 mL||0.42 mL||0.84 mL|
References are publications that support the biological activity of the product.
Wu et al (2022) NAMPT-targeting PROTAC promotes antitumor immunity via suppressing myeloid-derived suppressor cell expansion. Acta.Pharm.Sin.B 12 2859 PMID: 35755293
If you know of a relevant reference for NAMPT PROTAC® A7, please let us know.
Keywords: NAMPT PROTAC® A7, NAMPT PROTAC® A7 supplier, protacs, active, degraders, potent, selective, nicotinamide, phosphoribosyl, transferase, NAMPT, Degrader, antitumor, immunity, Active, Degraders, 7842, Tocris Bioscience
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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
This brochure highlights the tools and services available from Bio-Techne to support Targeted Protein Degradation research, including:
Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.
This poster summarizes the main epigenetic targets in cancer. The dysregulation of epigenetic modifications has been shown to result in oncogenesis and cancer progression. Unlike genetic mutations, epigenetic alterations are considered to be reversible and thus make promising therapeutic targets.
Degraders (e.g. PROTACs) are bifunctional small molecules, that harness the Ubiquitin Proteasome System (UPS) to selectively degrade target proteins within cells. They consist of three covalently linked components: an E3 ubiquitin ligase ligand, a linker and a ligand for the target protein of interest. Authored in-house, this poster outlines the generation of a toolbox of building blocks for the development of Degraders. The characteristics and selection of each of these components are discussed. Presented at EFMC 2018, Ljubljana, Slovenia