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903957

Sigma-Aldrich

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

别名:

(2S,4R)-1-((S)-2-(2-(2-Azidoethoxy)acetamido)-3,3-dimethylbutanoyl)-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）:
C26H35N7O5S
CAS号:
2101200-09-1
分子量:
557.67
MDL编号:
MFCD31807301
UNSPSC代码:
51171641
NACRES:
NA.22

ligand

VH032

方案

≥95%

表单

powder

反应适用性

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

官能团

azide

储存温度

2-8°C

SMILES字符串

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(COCCN=[N+]=[N-])=O)=O

InChI

1S/C26H35N7O5S/c1-16-22(39-15-29-16)18-7-5-17(6-8-18)12-28-24(36)20-11-19(34)13-33(20)25(37)23(26(2,3)4)31-21(35)14-38-10-9-30-32-27/h5-8,15,19-20,23,34H,9-14H2,1-4H3,(H,28,36)(H,31,35)/t19-,20+,23-/m1/s1

InChI key

YVCURZJBLHZABY-ZRCGQRJVSA-N

相关类别

应用

Protein degrader builiding block (S,R,S)-AHPC-PEG1-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 and a PEGylated crosslinker with pendant azide for click chemistry with 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 azide 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)

其他说明

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

法律信息

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

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Bromo-PEG2-acid, ≥95%

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Bromo-PEG3-acid

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Propargyl-PEG2-acid

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Pomalidomide-PEG6-CO2H

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Pomalidomide-PEG5-CO2H, ≥95%

901824

Pomalidomide-PEG4-CO2H

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(S,R,S)-AHPC-PEG6-NH2 hydrochloride, ≥95%

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

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储存分类代码

11 - Combustible Solids

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

历史批次信息供参考:

分析证书(COA)

Lot/Batch Number
0000145450
0000104550
MKCJ0500

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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.

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