所有图片(1)

Key Documents

905402

(S,R,S)-AHPC-C₆-PEG₁-C₃-PEG₁-butyl chloride

Name: (S,R,S)-AHPC-C6-PEG1-C3-PEG1-butyl chloride
Brand: ALDRICH

95%

别名:

(2S,4R)-1-((S)-2-(6-((5-((6-Chlorohexyl)oxy)pentyl)oxy)hexanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide, (S,R,S)-AHPC-6-5-6-Cl, 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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所有图片(1)

About This Item

经验公式（希尔记法）:

C₃₉H₆₁ClN₄O₆S

CAS号:

1835705-61-7

分子量:

749.44

MDL號碼:

MFCD31560481

分類程式碼代碼:

12352101

ligand

VH032

化驗

95%

形狀

solid

反應適用性

reactivity: sulfuryl reactive
reagent type: ligand-linker conjugate

官能基

alkyl halide

儲存溫度

2-8°C

SMILES 字串

ClCCCCCCOCCCCCOCCCCCC(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)=O

應用

Protein degrader builiding block (S,R,S)-AHPC-C₆-PEG₁-C₃-PEG₁-butyl Chloride 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 chloroalkane for reactivity with a nucleophilic group on a 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 chloro 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

Modular PROTAC Design for the Degradation of Oncogenic BCR-ABL

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

13 - Non Combustible Solids

水污染物質分類（WGK）

WGK 3

閃點（°F）

Not applicable

閃點（°C）

Not applicable

从最新的版本中选择一种：

分析证书(COA)

Lot/Batch Number

MKCJ8294

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Sigma-Aldrich

901525

Pomalidomide-C₉-CO₂H

Sigma-Aldrich

901848

(S,R,S)-AHPC-PEG₄-NH₂ hydrochloride

Sigma-Aldrich

901511

(S,R,S)-AHPC-PEG₃-NH₂ hydrochloride

Sigma-Aldrich

901503

(S,R,S)-AHPC-PEG₁-Alkyne

Sigma-Aldrich

904651

(S,R,S)-AHPC-PEG₃-azide

Sigma-Aldrich

901533

(S,R,S)-AHPC-PEG₃-Alkyne

Sigma-Aldrich

901860

(S,R,S)-AHPC-PEG₆-NH₂ hydrochloride

Modular PROTAC Design for the Degradation of Oncogenic BCR-ABL.

Ashton C Lai et al.

Angewandte Chemie (International ed. in English), 55(2), 807-810 (2015-11-26)

Proteolysis Targeting Chimera (PROTAC) technology is a rapidly emerging alternative therapeutic strategy with the potential to address many of the challenges currently faced in modern drug development programs. PROTAC technology employs small molecules that recruit target proteins for ubiquitination and

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

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-C6-PEG1-C3-PEG1-butyl chloride

95%

About This Item

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

相關產品

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-C₆-PEG₁-C₃-PEG₁-butyl chloride