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About This Item
Empirical Formula (Hill Notation):
C40H63ClN4O10S
CAS Number:
Molecular Weight:
827.47
MDL number:
UNSPSC Code:
12352101
ligand
VH032
form
liquid
reaction suitability
reactivity: sulfuryl reactive
reagent type: ligand-linker conjugate
functional group
alkyl halide
storage temp.
2-8°C
SMILES string
ClCCCCCCOCCOCCOCCOCCOCCOCC(N[C@H](C(N1[C@H](C(NCC2=CC=C(C3=C(C)N=CS3)C=C2)=O)C[C@@H](O)C1)=O)C(C)(C)C)=O
Application
Protein degrader builiding block (S,R,S)-AHPC-PEG6-Butyl chloride 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, a linker with both hydrophobic and hydrophilic moieties, and a pendant chloroalkane for reactivity with a nucleophilic group on a 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 pendant chloro group, parallel synthesis can be used to more quickly generate PROTAC libraries that feature variation in crosslinker length, composition, and E3 ligase ligand.
Other Notes
Technology Spotlight: Degrader Building Blocks for Targeted Protein Degradation.
Portal: Building PROTAC® Degraders for Targeted Protein Degradation
Targeted Protein Degradation by Small Molecules
Small-Molecule PROTACS: New Approaches to Protein Degradation
Targeted Protein Degradation: from Chemical Biology to Drug Discovery
Impact of linker length on the activity of PROTACs
Modular PROTAC Design for the Degradation of Oncogenic BCR-ABL
Portal: Building PROTAC® Degraders for Targeted Protein Degradation
Targeted Protein Degradation by Small Molecules
Small-Molecule PROTACS: New Approaches to Protein Degradation
Targeted Protein Degradation: from Chemical Biology to Drug Discovery
Impact of linker length on the activity of PROTACs
Modular PROTAC Design for the Degradation of Oncogenic BCR-ABL
Legal Information
PROTAC is a registered trademark of Arvinas Operations, Inc., and is used under license
Storage Class Code
10 - Combustible liquids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
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