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Sigma-Aldrich

Pomalidomide-piperazine-piperidine-4-carboxamide hydrochloride

Sinônimo(s):

2-(2,6-Dioxopiperidin-3-yl)-4-(4-(piperidine-4-carbonyl)piperazin-1-yl)isoindoline-1,3-dione hydrochloride, Crosslinker−E3 ligase ligand conjugate, Protein degrader building block

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About This Item

Fórmula empírica (Notação de Hill):
C23H27N5O5 · xHCl
Peso molecular:
453.49 (free base basis)

adequação da reação

reactivity: carboxyl reactive
reagent type: ligand-linker conjugate

Nível de qualidade

100

grupo funcional

amine

temperatura de armazenamento

2-8°C

cadeia de caracteres SMILES

O=C1C(N2C(C(C=CC=C3N4CCN(C(C5CCNCC5)=O)CC4)=C3C2=O)=O)CCC(N1)=O.Cl

Categorias relacionadas

Aplicação

Protein degrader building block Pomalidomide-piperazine-piperidine-4-carboxamide hydrochloride enables the synthesis of molecules for targeted protein degradation and PROTAC® (proteolysis-targeting chimeras) research. This conjugate contains a Cereblon (CRBN) recruiting ligand, 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 degrader, many analogs are prepared to screen for optimal target degradation. When used with other protein degrader building blocks with a terminal amine, parallel synthesis can be used to more quickly generate degrader libraries that feature variation in crosslinker length, composition, and E3 ligase ligand.

Technology Spotlight: Degrader Building Blocks for Targeted Protein Degradation

Protein Degrader Building Blocks

Outras notas

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

Pictogramas

Health hazard
GHS08

Palavra indicadora

Danger

Frases de perigo

H360D

Classificações de perigo

Repr. 1B

Código de classe de armazenamento

6.1C - Combustible, acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects

Classe de risco de água (WGK)

WGK 3

Ponto de fulgor (°F)

Not applicable

Ponto de fulgor (°C)

Not applicable

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Daniel P Bondeson et al.
Annual review of pharmacology and toxicology, 57, 107-123 (2016-10-13)
Protein homeostasis networks are highly regulated systems responsible for maintaining the health and productivity of cells. Whereas therapeutics have been developed to disrupt protein homeostasis, more recently identified techniques have been used to repurpose homeostatic networks to effect degradation of

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