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919896

Sigma-Aldrich

C5 Lenalidomide-dipiperazine-NH2 hydrochloride

Sinonimo/i:

4-(4-(2-Aminoethyl)piperazine-1-carbonyl)-N-(2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-5-yl)piperazine-1-carboxamide, C5 Lenalidomide conjugate, 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):
C25H34N8O5 · xHCl
Peso molecolare:
526.59 (free base basis)
Codice UNSPSC:
12352101
NACRES:
NA.22

ligand

C5 Lenalidomide

Livello qualitativo

100

Forma fisica

solid

Impiego in reazioni chimiche

reactivity: carboxyl reactive
reagent type: ligand-linker conjugate

Temperatura di conservazione

2-8°C

Stringa SMILE

O=C(N(CC1)CCN1C(NC2=CC(C3)=C(C=C2)C(N3C(C4=O)CCC(N4)=O)=O)=O)N5CCN(CC5)CCN.Cl

Applicazioni

Protein degrader building block C5 Lenalidomine-dipiperazine-NH2 hydrochloride enables the synthesis of molecules for targeted protein degradation and PROTAC (proteolysis-targeting chimeras) technology. This conjugate contains a Cereblon (CRBN)-recruiting ligand with alternative exit vector, a rigid linker, 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

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

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Classe di pericolosità dell'acqua (WGK)

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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..

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