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909262

(S,R,S)-AHPC-PEG₄-Azide

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

≥95%

别名:

(2S,4R)-1-((S)-17-Azido-2-(tert-butyl)-4-oxo-6,9,12,15-tetraoxa-3-azaheptadecanoyl)-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

经验公式（希尔记法）:

C₃₂H₄₇N₇O₈S

CAS号:

1797406-81-5

分子量:

689.82

分類程式碼代碼:

51171641

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Slide 1 of 10

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Sigma-Aldrich

904651

(S,R,S)-AHPC-PEG₃-azide

Sigma-Aldrich

245054

甲基三苯基碘化膦

Sigma-Aldrich

903957

(S,R,S)-AHPC-PEG1-azide

Sigma-Aldrich

901855

(S,R,S)-AHPC-PEG₅-Alkyne

Sigma-Aldrich

415952

(2,4,6-三甲基苯甲酰基)二苯基氧化膦

Sigma-Aldrich

SAB5801060

Goat Anti-Rabbit IgG(Fcγ) HRP Alpaca Heavy chain only Antibody

Sigma-Aldrich

216666

四(三苯基膦)钯(0)

Sigma-Aldrich

436909

二脲烷二甲基丙烯酸酯，异构体混合物

Sigma-Aldrich

923192

Spiro-TTB

Sigma-Aldrich

L9504

D -荧光素

ligand

VH032

化驗

≥95%

形狀

liquid

反應適用性

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

官能基

azide

儲存溫度

2-8°C

SMILES 字串

O=C(COCCOCCOCCOCCN=[N+]=[N-])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-Azide 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 azide for click chemistry with an alkyne 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 azide 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 Target Warhead and Linkage Vector on Inducing Protein Degradation: Comparison of Bromodomain and Extra-Terminal (BET) Degraders Derived from Triazolodiazepine (JQ1) and Tetrahydroquinoline (I-BET726) BET Inhibitor Scaffolds

Selective Small Molecule Induced Degradation of the BET Bromodomain Protein BRD4

法律資訊

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

儲存類別代碼

10 - Combustible liquids

水污染物質分類（WGK）

WGK 3

閃點（°F）

Not applicable

閃點（°C）

Not applicable

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分析证书(COA)

Lot/Batch Number

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Impact of Target Warhead and Linkage Vector on Inducing Protein Degradation: Comparison of Bromodomain and Extra-Terminal (BET) Degraders Derived from Triazolodiazepine (JQ1) and Tetrahydroquinoline (I-BET726) BET Inhibitor Scaffolds.

Kwok-Ho Chan et al.

Journal of medicinal chemistry, 61(2), 504-513 (2017-06-09)

The design of proteolysis-targeting chimeras (PROTACs) is a powerful small-molecule approach for inducing protein degradation. PROTACs conjugate a target warhead to an E3 ubiquitin ligase ligand via a linker. Here we examined the impact of derivatizing two different BET bromodomain

Selective Small Molecule Induced Degradation of the BET Bromodomain Protein BRD4.

Michael Zengerle et al.

ACS chemical biology, 10(8), 1770-1777 (2015-06-03)

The Bromo- and Extra-Terminal (BET) proteins BRD2, BRD3, and BRD4 play important roles in transcriptional regulation, epigenetics, and cancer and are the targets of pan-BET selective bromodomain inhibitor JQ1. However, the lack of intra-BET selectivity limits the scope of current

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

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

商品

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.

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.

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Key Documents

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

≥95%

About This Item

推荐产品

属性

ligand

化驗

形狀

反應適用性

官能基

儲存溫度

SMILES 字串

说明

應用

其他說明

法律資訊

相关产品

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安全信息

儲存類別代碼

水污染物質分類（WGK）

閃點（°F）

閃點（°C）

文件

分析证书(COA)

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(S,R,S)-AHPC-PEG₄-Azide