跳转至内容
Merck
CN

主要文件

查看所有文档

901503

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

≥95%

别名:

(2S,4R)-1-((S)-3,3-Dimethyl-2-(3-(prop-2-yn-1-yloxy)propanamido)butanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide, CrosslinkerE3 Ligase ligand conjugate, Protein degrader building block for PROTAC® research, Template for synthesis of targeted protein degrader, VH032 conjugate

登录 查看组织和合同定价。

选择尺寸

变更视图

关于此项目

经验公式（希尔记法）:
C28H36N4O5S
分子量:
540.67
MDL number:
MFCD32173778
UNSPSC Code:
51171641
NACRES:
NA.22
技术服务
需要帮助？我们经验丰富的科学家团队随时乐意为您服务。
让我们为您提供帮助

ligand

VH032

Quality Level

100

assay

≥95%

form

powder or crystals

reaction suitability

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

functional group

alkyne

storage temp.

2-8°C

SMILES string

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(CCOCC#C)=O)=O

InChI key

AFKRHNLUPSUNPJ-OTNCWRBYSA-N

Application

Protein degrader builiding block (S,R,S)-AHPC-PEG1-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)

Other Notes

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

Legal Information

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

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

历史批次信息供参考:

分析证书(COA)

Lot/Batch Number

It looks like we've run into a problem, but you can still download Certificates of Analysis from our 文件 section.

如需帮助，请联系 客户支持

已有该产品？

在文件库中查找您最近购买产品的文档。

访问文档库

商品

Degrader Building Blocks for Targeted Protein Degradation

Protein Degrader Building Blocks are a collection of crosslinker-E3 ligand conjugates with a pendant functional group for covalent linkage to a target ligand.

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
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
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
查看所有相关文献

全球贸易项目编号

货号GTIN
901503-50MG04061834671596