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安全信息

910597

Sigma-Aldrich

(S,R,S)-AHPC-PEG6-butyl alkyne

≥95%

别名:

(2S,4R)-1-((S)-2-(tert-Butyl)-4-oxo-6,9,12,15,18,21-hexaoxa-3-azanonacos-28-ynoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide, (S,R,S)-AHPC-2-2-2-2-2-2-6-alkyne, Crosslinker−E3 Ligase ligand conjugate, Protein degrader building block for PROTAC® research, Template for synthesis of targeted protein degrader, VH032 conjugate

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About This Item

经验公式（希尔记法）:
C42H64N4O10S
分子量:
817.04
UNSPSC代码:
51171641

ligand

VH032

检测方案

≥95%

形式

(Liquid or Semi-Solid or Paste or Solid)

反应适用性

reaction type: click chemistry
reagent type: ligand-linker conjugate

官能团

alkyne

储存温度

2-8°C

SMILES字符串

O=C(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)COCCOCCOCCOCCOCCOCCCCCCC#C

应用

Protein degrader builiding block (S,R,S)-AHPC-PEG6-butyl alkyne 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 alkyne for click chemistry with an azide 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 pendant alkyne group, parallel synthesis can be used to more quickly generate PROTAC libraries that feature variation in crosslinker length, composition, and E3 ligase ligand.

其他说明

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

法律信息

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

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WGK

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闪点(°F)

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闪点(°C)

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法规信息

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商品

Degrader Building Blocks for Targeted Protein Degradation

Protein Degrader Building Blocks are a collection of crosslinker-E3 ligand conjugates with a pendant functional group for covalent linkage to a target ligand.

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