NAMPT PROTAC® A7

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Description: Potent and selective nicotinamide phosphoribosyl transferase (NAMPT) Degrader (PROTAC®)
Chemical Name: (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-carboxamide
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (2)

Biological Activity for NAMPT PROTAC® A7

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.

Antibodies validated for Simple Western™ (automated Western) instruments and Western Blot also available: Catalog # AF4335 and MAB40441.

PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.

Technical Data for NAMPT PROTAC® A7

M. Wt 1185.49
Formula C58H76N10O11S3
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 2484876-94-8
InChI Key WJRWRYBOCSUYIN-IWIXZVHYSA-N
Smiles O=C(C1=CC=C(C=C1)CN2CCN(CC2)S(=O)(C3=CC=C(C=C3)NC(NCC4=CN=CC=C4)=S)=O)NCCOCCOCCOCCOCC(N[C@@H](C(C)(C)C)C(N5[C@@H](C[C@H](C5)O)C(N[C@H](C6=CC=C(C7=C(N=CS7)C)C=C6)C)=O)=O)=O

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.

Solubility Data for NAMPT PROTAC® A7

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 23.71 20

Preparing Stock Solutions for NAMPT PROTAC® A7

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.

Select a batch to recalculate based on the batch molecular weight:
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

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Product Datasheets for NAMPT PROTAC® A7

References for NAMPT PROTAC® A7

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.

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Keywords: NAMPT PROTAC® A7, NAMPT PROTAC® A7 supplier, protacs, active, degraders, potent, selective, nicotinamide, phosphoribosyl, transferase, NAMPT, Degrader, antitumor, immunity, Other, Degraders, 7842, Tocris Bioscience

Citations for NAMPT PROTAC® A7

Citations are publications that use Tocris products.

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Literature in this Area

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Targeted Protein Degradation Research Product Guide

Targeted Protein Degradation Research Product Guide

This brochure highlights the tools and services available from Bio-Techne to support Targeted Protein Degradation research, including:

  • Active Degraders
  • TAG Degradation Platform
  • Degrader Building Blocks
  • Ubiquitin-Proteasome System Proteins
  • Assays for Protein Degradation
Targeted Protein Degradation Poster

Targeted Protein Degradation Poster

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