Accéder au contenu
Merck
Toutes les photos(1)

Key Documents

View All Documentation

923877

Sigma-Aldrich

Pomalidomide-piperazine-C1-4-piperidine hydrochloride

Synonyme(s) :

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

Se connecterpour consulter vos tarifs contractuels et ceux de votre entreprise/organisme
Toutes les photos(1)

About This Item

Formule empirique (notation de Hill):
C23H29N5O4 · xHCl
Poids moléculaire :
439.51 (free base basis)
Nomenclature NACRES :
NA.21

ligand

pomalidomide

Niveau de qualité

100

Pertinence de la réaction

reactivity: carboxyl reactive
reagent type: ligand-linker conjugate

Groupe fonctionnel

amine

Température de stockage

2-8°C

Chaîne SMILES 

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

Application

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

Autres remarques

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

Informations légales

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

Produit(s) apparenté(s)

Réf. du produit
Description
Tarif

911771

Lenalidomide-Photoswitch1-NH2 hydrochloride, ≥95%

911763

C5 Lenalidomide-PEG1-piperazine hydrochloride, ≥95%

915572

Pomalidomide-dipiperazine-NH2 hydrochloride, ≥95%

916536

Pomalidomide-piperazine-pyridine-alkyne-NH2 hydrochloride

917729

C5 Lenalidomide-piperazine-pyridine-alkyne-NH2 hydrochloride, ≥95%

919357

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

918350

C5 Lenalidomide-alkyne-piperidine hydrochloride, ≥95%

918687

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

919896

C5 Lenalidomide-dipiperazine-NH2 hydrochloride

920606

(S,R,S)-AHPC-piperazine-pyridine-alkyne-NH2 hydrochloride

920746

Pomalidomide-benzyl-piperazine hydrochloride

920762

(S,R,S)-AHPC-benzyl-piperazine hydrochloride

920754

C5 Lenalidomide-benzyl-piperazine hydrochloride

920789

Pomalidomide-pyridine-PEG1-piperazine hydrochloride

920797

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

920800

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

920843

(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

922153

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

922161

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

921939

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

Pictogrammes

Health hazard
GHS08

Mention d'avertissement

Danger

Mentions de danger

H360D

Classification des risques

Repr. 1B

Code de la classe de stockage

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

Classe de danger pour l'eau (WGK)

WGK 3

Point d'éclair (°F)

Not applicable

Point d'éclair (°C)

Not applicable

Faites votre choix parmi les versions les plus récentes :

Certificats d'analyse (COA)

Lot/Batch Number

Désolés, nous n'avons pas de COA pour ce produit disponible en ligne pour le moment.

Si vous avez besoin d'assistance, veuillez contacter Service Clients

Déjà en possession de ce produit ?

Retrouvez la documentation relative aux produits que vous avez récemment achetés dans la Bibliothèque de documents.

Consulter la Bibliothèque de documents

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

Articles

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.

Notre équipe de scientifiques dispose d'une expérience dans tous les secteurs de la recherche, notamment en sciences de la vie, science des matériaux, synthèse chimique, chromatographie, analyse et dans de nombreux autres domaines..

Contacter notre Service technique