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920789

Sigma-Aldrich

Pomalidomide-pyridine-PEG1-piperazine hydrochloride

Sinonimo/i:

N-(2-(2,6-Dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)-2-(6-(3-(piperazin-1-yl)propoxy)pyridin-3-yl)acetamide hydrochloride, 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

Formula empirica (notazione di Hill):
C27H30N6O6 · xHCl
Peso molecolare:
534.56 (free base basis)
NACRES:
NA.22

ligand

pomalidomide

Livello qualitativo

100

Forma fisica

powder or crystals

Impiego in reazioni chimiche

reactivity: carboxyl reactive
reagent type: ligand-linker conjugate

Gruppo funzionale

amine

Temperatura di conservazione

2-8°C

Stringa SMILE

O=C(N(C1CCC(NC1=O)=O)C2=O)C3=C2C=CC=C3NC(CC4=CC=C(OCCCN5CCNCC5)N=C4)=O.Cl

Applicazioni

Protein degrader building block Pomalidomide-pyridine-PEG1-piperazine hydrochloride enables the synthesis of molecules for targeted protein degradation and PROTAC (proteolysis-targeting chimeras) technology. This conjugate contains a Cereblon (CRBN)-recruiting ligand, a linker with added rigidity, and a pendant amine for reactivity with a carboxylic acid 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.

Altre note

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

Note legali

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

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Codice della classe di stoccaggio

11 - Combustible Solids

Classe di pericolosità dell'acqua (WGK)

WGK 3

Punto d’infiammabilità (°F)

Not applicable

Punto d’infiammabilità (°C)

Not applicable

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Articoli

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.

Il team dei nostri ricercatori vanta grande esperienza in tutte le aree della ricerca quali Life Science, scienza dei materiali, sintesi chimica, cromatografia, discipline analitiche, ecc..

Contatta l'Assistenza Tecnica.