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923877

Sigma-Aldrich

Pomalidomide-piperazine-C1-4-piperidine hydrochloride

Sinónimos:

2-(2,6-Dioxopiperidin-3-yl)-4-(4-(piperidin-4-ylmethyl)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 (notación de Hill):
C23H29N5O4 · xHCl
Peso molecular:
439.51 (free base basis)
NACRES:
NA.21

ligand

pomalidomide

Nivel de calidad

100

idoneidad de la reacción

reactivity: carboxyl reactive
reagent type: ligand-linker conjugate

grupo funcional

amine

temp. de almacenamiento

2-8°C

cadena SMILES

O=C1C(N2C(C(C=CC=C3N4CCN(CC5CCNCC5)CC4)=C3C2=O)=O)CCC(N1)=O.Cl

Aplicación

Protein degrader building block Pomalidomide-piperazine-C1-4-piperidine 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

Otras 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

Información legal

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

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Descripción
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Pomalidomide-piperazine-pyridine-alkyne-NH2 hydrochloride

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(S,R,S)-AHPC-PEG1-piperazine hydrochloride, ≥95%

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(S,R,S)-AHPC-alkyne-piperidine hydrochloride

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C5 Lenalidomide-benzyl-piperazine hydrochloride

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Pomalidomide-pyridine-PEG1-piperazine hydrochloride

920797

C5 Lenalidomide-pyridine-PEG1-piperazine hydrochloride, ≥95%

920800

C5 Lenalidomide-methylamino-PEG1-NH2 hydrochloride, ≥95%

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(S,R,S)-VL285 Phenol-PEG1-piperazine hydrochloride

920827

(S,R,S)-AHPC-methylamino-PEG1-NH2 hydrochloride

921300

C5 Lenalidomide-pyrimidine-piperazine-PEG1-NH2 hydrochloride, ≥95%

921319

Pomalidomide-methylamino-PEG1-NH2 hydrochloride

921432

(S,R,S)-AHPC-pyridine-PEG1-piperazine hydrochloride

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(S,R,S)-VL285 Phenol-C3-piperazine hydrochloride

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(S,R,S)-VL285 Phenol-methylamino-PEG1-NH2 hydrochloride

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(S,R,S)-AHPC-pyrimidine-piperazine-PEG1-NH2 hydrochloride

Pictogramas

Health hazard
GHS08

Palabra de señalización

Danger

Frases de peligro

H360D

Clasificaciones de peligro

Repr. 1B

Código de clase de almacenamiento

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

Clase de riesgo para el agua (WGK)

WGK 3

Punto de inflamabilidad (°F)

Not applicable

Punto de inflamabilidad (°C)

Not applicable

Certificados de análisis (COA)

Busque Certificados de análisis (COA) introduciendo el número de lote del producto. Los números de lote se encuentran en la etiqueta del producto después de las palabras «Lot» o «Batch»

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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
Kedra Cyrus et al.
Molecular bioSystems, 7(2), 359-364 (2010-10-06)
Conventional genetic approaches have provided a powerful tool in the study of proteins. However, these techniques often preclude selective manipulation of temporal and spatial protein functions, which is crucial for the investigation of dynamic cellular processes. To overcome these limitations
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
Momar Toure et al.
Angewandte Chemie (International ed. in English), 55(6), 1966-1973 (2016-01-13)
The current inhibitor-based approach to therapeutics has inherent limitations owing to its occupancy-based model: 1) there is a need to maintain high systemic exposure to ensure sufficient in vivo inhibition, 2) high in vivo concentrations bring potential for off-target side effects, and 3) there is

Artículos

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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