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資料

901517

(S,R,S)-AHPC-PEG₂-Alkyne

Name: (S,R,S)-AHPC-PEG2-Alkyne
Brand: ALDRICH

≥95%

別名:

(2S,4R)-1-((S)-3,3-Dimethyl-2-(3-(2-(prop-2-yn-1-yloxy)ethoxy)propanamido)butanoyl)-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

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About This Item

実験式（ヒル表記法）:

C₃₀H₄₀N₄O₆S

分子量:

584.73

UNSPSCコード:

51171641

NACRES:

NA.22

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Sigma-Aldrich

901855

(S,R,S)-AHPC-PEG₅-Alkyne

Sigma-Aldrich

901503

(S,R,S)-AHPC-PEG₁-Alkyne

Sigma-Aldrich

904651

(S,R,S)-AHPC-PEG₃-azide

Sigma-Aldrich

764205

アルキン-PEG4-マレイミド

Sigma-Aldrich

903434

Pomalidomide-PEG₆-butyl azide

Sigma-Aldrich

901531

Pomalidomide-PEG₃-Alkyne

Sigma-Aldrich

JKA4095

Alkyne-PEG5K-Alkyne

Sigma-Aldrich

900602

4-(4-(Prop-2-yn-1-yloxy)benzoyl)benzoic acid

Sigma-Aldrich

901523

Pomalidomide-PEG₁-Alkyne

品質水準

100

アッセイ

≥95%

形状

powder

反応適合性

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

官能基

alkyne

保管温度

2-8°C

SMILES記法

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(CCOCCOCC#C)=O)=O

アプリケーション

Protein degrader builiding block (S,R,S)-AHPC-PEG₂-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)

その他情報

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

法的情報

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

保管分類コード

11 - Combustible Solids

WGK

WGK 3

引火点(°F)

Not applicable

引火点(℃)

Not applicable

試験成績書（COA）

製品のロット番号・バッチ番号を入力して、試験成績書（COA）を検索できます。ロット番号・バッチ番号は、製品ラベルに「Lot」または「Batch」に続いて記載されています。

以前この製品を購入いただいたことがある場合

文書ライブラリで、最近購入した製品の文書を検索できます。

文書ライブラリにアクセスする

Small-Molecule PROTACS: New Approaches to Protein Degradation.

Momar Toure et al.

Angewandte Chemie (International ed. in English), 55(6), 1966-1973 (2016-01-13)

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

Impact of linker length on the activity of PROTACs.

Kedra Cyrus et al.

Molecular bioSystems, 7(2), 359-364 (2010-10-06)

Conventional genetic approaches have provided a powerful tool in the study of proteins. However, these techniques often preclude selective manipulation of temporal and spatial protein functions, which is crucial for the investigation of dynamic cellular processes. To overcome these limitations

Targeted Protein Degradation: from Chemical Biology to Drug Discovery.

Philipp M Cromm et al.

Cell chemical biology, 24(9), 1181-1190 (2017-06-27)

Traditional pharmaceutical drug discovery is almost exclusively focused on directly controlling protein activity to cure diseases. Modulators of protein activity, especially inhibitors, are developed and applied at high concentration to achieve maximal effects. Thereby, reduced bioavailability and off-target effects can

Targeted Protein Degradation by Small Molecules.

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

資料

Degrader Building Blocks for Targeted Protein Degradation

Partial PROTACs are a collection of crosslinker-E3 ligand conjugates with a pendant functional group for covalent linkage to a target ligand.

Partial PROTACs for Targeted Protein Degradation

Partial PROTACs are a collection of crosslinker-E3 ligand conjugates with a pendant functional group for covalent linkage to a target ligand.

ライフサイエンス、有機合成、材料科学、クロマトグラフィー、分析など、あらゆる分野の研究に経験のあるメンバーがおります。.

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資料

(S,R,S)-AHPC-PEG2-Alkyne

≥95%

About This Item

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特性

品質水準

アッセイ

形状

反応適合性

官能基

保管温度

SMILES記法

関連するカテゴリー

詳細

アプリケーション

その他情報

法的情報

関連製品

関連製品

安全性情報

保管分類コード

WGK

引火点(°F)

引火点(℃)

資料

試験成績書（COA）

以前この製品を購入いただいたことがある場合

参考文献

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資料

テクニカルサービス

(S,R,S)-AHPC-PEG₂-Alkyne