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Key Documents

原産地証明書（COO）/試験成績書（COA）

データシートなど

安全性情報

適用法令

901860

(S,R,S)-AHPC-PEG₆-NH₂ hydrochloride

Name: (S,R,S)-AHPC-PEG6-NH2 hydrochloride
Brand: ALDRICH

≥95%

別名:

(2S,4R)-1-((S)-23-Amino-2-(tert-butyl)-4-oxo-6,9,12,15,18,21-hexaoxa-3-azatricosanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide hydrochloride, 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

実験式（ヒル表記法）:

C₃₆H₅₈ClN₅O₁₀S

分子量:

788.39

UNSPSCコード:

12352101

NACRES:

NA.22

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Sigma-Aldrich

901493

(S,R,S)-AHPC-PEG₁-NH₂ hydrochloride

Sigma-Aldrich

901488

(S,R,S)-AHPC-PEG₂-NH₂ hydrochloride

Sigma-Aldrich

901831

Pomalidomide-PEG₅-NH₂hydrochloride

Sigma-Aldrich

901511

(S,R,S)-AHPC-PEG₃-NH₂ hydrochloride

Sigma-Aldrich

901490

(S,R,S)-AHPC hydrochloride

Sigma-Aldrich

920908

(S,R,S)-VL285 Phenol

Sigma-Aldrich

920606

(S,R,S)-AHPC-piperazine-pyridine-alkyne-NH₂ hydrochloride

Sigma-Aldrich

901830

Pomalidomide-PEG₄-NH₂ hydrochloride

Sigma-Aldrich

901848

(S,R,S)-AHPC-PEG₄-NH₂ hydrochloride

Sigma-Aldrich

901565

Propargyl-PEG₃-acid

ligand

VH032

アッセイ

≥95%

形状

powder or crystals

反応適合性

reactivity: carboxyl reactive
reagent type: ligand-linker conjugate

官能基

amine

保管温度

2-8°C

SMILES記法

O=C(COCCOCCOCCOCCOCCOCCN)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.Cl

アプリケーション

Protein degrader building block (S,R,S)-AHPC-PEG₆-NH₂ (HCL salt) 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 amine for reactivity with a carboxyl group 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 amine, 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

適用法令

試験研究用途を考慮した関連法令を主に挙げております。化学物質以外については、一部の情報のみ提供しています。製品を安全かつ合法的に使用することは、使用者の義務です。最新情報により修正される場合があります。WEBの反映には時間を要することがあるため、適宜SDSをご参照ください。

Jan Code

901860-VAR:
901860-50MG:
901860-BULK:

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

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.

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.

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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Key Documents

安全性情報

(S,R,S)-AHPC-PEG6-NH2 hydrochloride

≥95%

About This Item

おすすめの製品

特性

ligand

アッセイ

形状

反応適合性

官能基

保管温度

SMILES記法

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

(S,R,S)-AHPC-PEG₆-NH₂ hydrochloride