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901533

(S,R,S)-AHPC-PEG₃-Alkyne

Name: (S,R,S)-AHPC-PEG3-Alkyne
Brand: ALDRICH

≥95%

同義詞:

(2S,4R)-1-((S)-2-(tert-Butyl)-4-oxo-7,10,13-trioxa-3-azahexadec-15-ynoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide, 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

經驗公式（希爾表示法）:

C₃₂H₄₄N₄O₇S

CAS號碼:

2374122-30-0

分子量：:

628.78

分類程式碼代碼:

51171641

NACRES:

NA.22

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Sigma-Aldrich

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(S,R,S)-AHPC-PEG₁-Alkyne

$(1 R ,8 S ,9 S )-二环 \ [6.1.0] 非-4-炔-9-基甲醇 for Copper-free Click Chemistry$

Sigma-Aldrich

742678

(1 R ,8 S ,9 S )-二环 \ [6.1.0] 非-4-炔-9-基甲醇

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QBD11205

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901490

(S,R,S)-AHPC hydrochloride

Sigma-Aldrich

901855

(S,R,S)-AHPC-PEG₅-Alkyne

Sigma-Aldrich

901534

(S,R,S)-AHPC-C₆-CO₂H hydrochloride

Sigma-Aldrich

901523

Pomalidomide-PEG₁-Alkyne

Sigma-Aldrich

901511

(S,R,S)-AHPC-PEG₃-NH₂ hydrochloride

Sigma-Aldrich

761540

二苯并环辛炔胺

ligand

VH032

品質等級

100

化驗

≥95%

形狀

powder or crystals

反應適用性

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

官能基

alkyne

儲存溫度

2-8°C

SMILES 字串

O=C(NCC1=CC=C(C2=C(C)N=CS2)C=C1)[C@H](C[C@@H](O)C3)N3C([C@H](C(C)(C)C)NC(CCOCCOCCOCC#C)=O)=O

應用

Protein degrader builiding block (S,R,S)-AHPC-PEG4-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 and a PEGylated crosslinker with 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.

Automate your VHL-PEG based PROTACs with Synple Automated Synthesis Platform (SYNPLE-SC002)

其他說明

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

法律資訊

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

儲存類別代碼

11 - Combustible Solids

水污染物質分類（WGK）

WGK 3

閃點（°F）

Not applicable

閃點（°C）

Not applicable

分析證明 (COA)

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The current inhibitor-based approach to therapeutics has inherent limitations owing to its occupancy-based model: 1) there is a need to maintain high systemic exposure to ensure sufficient in vivo inhibition, 2) high in vivo concentrations bring potential for off-target side effects, and 3) there is

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文章

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(S,R,S)-AHPC-PEG3-Alkyne

≥95%

About This Item

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屬性

ligand

品質等級

化驗

形狀

反應適用性

官能基

儲存溫度

SMILES 字串

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描述

應用

其他說明

法律資訊

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儲存類別代碼

水污染物質分類（WGK）

閃點（°F）

閃點（°C）

文件

分析證明 (COA)

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(S,R,S)-AHPC-PEG₃-Alkyne