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901828

Sigma-Aldrich

Pomalidomide-PEG5-CO2H

≥95%

Sinônimo(s):

1-((2-(2,6-Dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)-3,6,9,12,15-pentaoxaoctadecan-18-oic acid, Crosslinker−E3 Ligase ligand conjugate, Protein degrader building block for PROTAC® research, Template for synthesis of targeted protein degrader

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About This Item

Fórmula empírica (Notação de Hill):
C26H35N3O11
Número CAS:
2139348-63-1
Peso molecular:
565.57
Código UNSPSC:
51171641
NACRES:
NA.22

ligand

pomalidomide

Ensaio

≥95%

forma

solid

adequação da reação

reactivity: amine reactive
reagent type: ligand-linker conjugate

grupo funcional

carboxylic acid

temperatura de armazenamento

2-8°C

cadeia de caracteres SMILES

O=C(C(CC1)N(C2=O)C(C3=C2C=CC=C3NCCOCCOCCOCCOCCOCCC(O)=O)=O)NC1=O

Aplicação

Protein degrader builiding block Pomalidomide-PEG5-CO2H enables the synthesis of molecules for targeted protein degradation and PROTAC (proteolysis-targeting chimeras) technology. This conjugate contains a Cereblon (CRBN)-recruiting ligand and a PEGylated crosslinker with pendant carboxylic acid for reactivity with an amine 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 carboxyl 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 CRBN-PEG based PROTACs with Synple Automated Synthesis Platform (SYNPLE-SC002)

Outras notas

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

Informações legais

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

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Código de classe de armazenamento

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Classe de risco de água (WGK)

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Ponto de fulgor (°C)

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Certificados de análise (COA)

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Momar Toure et al.
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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

Artigos

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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