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901851

(S,R,S)-AHPC-PEG₄-Alkyne

Name: (S,R,S)-AHPC-PEG4-Alkyne
Brand: ALDRICH

同義詞:

(2S,4R)-1-((S)-2-(tert-Butyl)-4-oxo-7,10,13,16-tetraoxa-3-azanonadec-18-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

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About This Item

經驗公式（希爾表示法）:

C₃₄H₄₈N₄O₈S

分子量：:

672.83

分類程式碼代碼:

51171641

NACRES:

NA.22

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Sigma-Aldrich

QBD11812

DBCO-dPEG ^®₁₂-carboxyfluorescein

Sigma-Aldrich

760765

叠氮化物氟 488

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901503

(S,R,S)-AHPC-PEG₁-Alkyne

Sigma-Aldrich

760757

5-羧基四甲基罗丹明-叠氮化物染料

Sigma-Aldrich

756598

聚氧乙烯二叠氮化物

Sigma-Aldrich

764205

炔-PEG4-马来酰亚胺

Sigma-Aldrich

776130

3-叠氮基-1-丙醇

Sigma-Aldrich

761621

Fluor 488-炔烃

Sigma-Aldrich

762024

N-[2-[2-[2-(2-叠氮乙氧基)乙氧基]乙氧基]乙基]生物素胺

Sigma-Aldrich

910147

Fluorescein Azide

ligand

VH032

形狀

solid

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(CCOCCOCCOCCOCC#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

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

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分析證明 (COA)

Lot/Batch Number

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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

文章

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.

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.

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Key Documents

(S,R,S)-AHPC-PEG4-Alkyne

About This Item

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屬性

ligand

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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安全資訊

儲存類別代碼

水污染物質分類（WGK）

閃點（°F）

閃點（°C）

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(S,R,S)-AHPC-PEG₄-Alkyne