920835
(S,R,S)-VL285 Phenol-piperazine-pyridine-alkyne-NH2 hydrochloride
Synonyme(s) :
(2S,4R)-N-{[2-(3-{4-[5-(3-Aminoprop-1-yn-1-yl)pyridin-2-yl]piperazin-1-yl}propoxy)-4-(4-methyl-1,3-thiazol-5-yl)phenyl]methyl}-4-hydroxy-1-[(2S)-3-methyl-2-(1-oxo-2,3-dihydro-1H-isoindol-2-yl)butanoyl]pyrrolidine-2-carboxamide hydrochloride, Crosslinker−E3 Ligase ligand conjugate, VHL protein degrader building block for PROTAC® research
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A propos de cet article
Formule empirique (notation de Hill) :
C44H52N8O5S · xHCl
Poids moléculaire :
805.00 (free base basis)
NACRES:
NA.22
UNSPSC Code:
12352101
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VL285 phenol
Quality Level
reaction suitability
reactivity: carboxyl reactive, reagent type: ligand-linker conjugate
functional group
amine
storage temp.
2-8°C
Application
Protein degrader building block (S,R,S)-VL285 Phenol-piperazine-pyridine-alkyne-NH2 hydrochloride enables the synthesis of molecules for targeted protein degradation and PROTAC (proteolysis-targeting chimeras) technology. This conjugate contains a von Hippel-Lindau (VHL)-recruiting ligand with alternative exit vector from the widely used VH032 (901490), a rigid inker, and a pendant amine for reactivity with a carboxylic acid on the target ligand. Because even slight alterations in ligands and crosslinkers can affect ternary complex formation between the target, E3 ligase, and PROTAC, many analogs are prepared to screen for optimal target degradation. When used with other protein degrader building blocks with a terminal amine, parallel synthesis can be used to more quickly generate PROTAC libraries that feature variation in crosslinker length, composition, and E3 ligase ligand.
Technology Spotlight: Degrader Building Blocks for Targeted Protein Degradation
Portal: Building PROTAC® Degraders for Targeted Protein Degradation
Technology Spotlight: Degrader Building Blocks for Targeted Protein Degradation
Portal: Building PROTAC® Degraders for Targeted Protein Degradation
Other Notes
Legal Information
PROTAC is a registered trademark of Arvinas Operations, Inc., and is used under license
wgk
WGK 3
Classe de stockage
11 - Combustible Solids
flash_point_f
Not applicable
flash_point_c
Not applicable
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Dennis L Buckley et al.
ACS chemical biology, 10(8), 1831-1837 (2015-06-13)
Small molecule-induced protein degradation is an attractive strategy for the development of chemical probes. One method for inducing targeted protein degradation involves the use of PROTACs, heterobifunctional molecules that can recruit specific E3 ligases to a desired protein of interest.
Daniel P Bondeson et al.
Annual review of pharmacology and toxicology, 57, 107-123 (2016-10-13)
Protein homeostasis networks are highly regulated systems responsible for maintaining the health and productivity of cells. Whereas therapeutics have been developed to disrupt protein homeostasis, more recently identified techniques have been used to repurpose homeostatic networks to effect degradation of
Numéro d'article de commerce international
| Référence | GTIN |
|---|---|
| 920835-50MG | 04065266438789 |