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Merck
CN

904651

(S,R,S)-AHPC-PEG3-azide

≥95%

别名:

(2S,4R)-1-((S)-14-azido-2-(tert-butyl)-4-oxo-6,9,12-trioxa-3-azatetradecanoyl)-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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关于此项目

经验公式（希尔记法）:
C30H43N7O7S
化学文摘社编号:
1797406-80-4
分子量:
645.77
MDL number:
MFCD31807299
UNSPSC Code:
51171641
NACRES:
NA.22

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产品名称

(S,R,S)-AHPC-PEG3-azide, ≥95%

InChI

1S/C30H43N7O7S/c1-20-26(45-19-33-20)22-7-5-21(6-8-22)16-32-28(40)24-15-23(38)17-37(24)29(41)27(30(2,3)4)35-25(39)18-44-14-13-43-12-11-42-10-9-34-36-31/h5-8,19,23-24,27,38H,9-18H2,1-4H3,(H,32,40)(H,35,39)/t23-,24+,27-/m1/s1

InChI key

MZOMHQGOVGODTD-ONBPZOJHSA-N

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

ligand

VH032

assay

≥95%

form

solid or liquid

reaction suitability

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

functional group

azide

storage temp.

2-8°C

相关类别

Application

Protein degrader building block (S,R,S)-AHPC-PEG3-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)

Other Notes

Technology Spotlight: Degrader Building Blocks for Targeted Protein Degradation

Portal: Building PROTAC® Degraders for Targeted Protein Degradation

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

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
0000103390
MKCJ1221

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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.

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