920835
(S,R,S)-VL285 Phenol-piperazine-pyridine-alkyne-NH2 hydrochloride
Synonym(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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About This Item
Empirical Formula (Hill Notation):
C44H52N8O5S · xHCl
Molecular Weight:
805.00 (free base basis)
NACRES:
NA.22
UNSPSC Code:
12352101
ligand
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
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Regulatory Information
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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.
Global Trade Item Number
| SKU | GTIN |
|---|---|
| 920835-50MG | 04065266438789 |