921939

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

• Synonim(y): 5-{4-[2-(2-Aminoethoxy)ethyl]piperazin-1-yl}-N-[(2R)-1-[(2R,4S)-4-hydroxy-2-({[4-(4-methyl-1,3-thiazol-5-yl)phenyl]methyl}carbamoyl)pyrrolidin-1-yl]-3,3-dimethyl-1-oxobutan-2-yl]pyrimidine-2-carboxamide hydrochloride, Crosslinker−E3 Ligase ligand conjugate, Protein degrader building block for PROTAC^® research, Template for synthesis of targeted protein degrader, VH032 conjugate
• Wzór empiryczny (zapis Hilla): C₃₅H₄₉N₉O₅S · xHCl
• Masa cząsteczkowa: 707.89 (free base basis)

Właściwości

• Postać: solid
• Poziom jakości: 100
• przydatność reakcji: reactivity: carboxyl reactive; reagent type: ligand-linker conjugate
• grupa funkcyjna: amine
• temp. przechowywania: 2-8°C
• ciąg SMILES: O=C([C@@H]1C[C@H](CN1C([C@H](C(C)(C)C)NC(C2=NC=C(C=N2)N3CCN(CC3)CCOCCN)=O)=O)O)NCC4=CC=C(C=C4)C5=C(N=CS5)C.[xHCl]

Opis

Zastosowanie

Protein degrader building block (S,R,S)-AHPC-pyrimidine-piperazine-PEG₁-NH₂ hydrochloride enables the synthesis of molecules for targeted protein degradation and PROTAC (proteolysis-targeting chimeras) technology. This conjugate contains a von Hippel–Lindau (VHL)-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 PROTAC, 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 PROTAC libraries that feature variation in crosslinker length, composition, and E3 ligase ligand.

Inne uwagi

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

Informacje prawne

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

This page may contain text that has been machine translated.

Informacja o środkach bezpieczeństwa

• Kod klasy składowania: 11 - Combustible Solids
• Klasa zagrożenia wodnego (WGK): WGK 3
• Temperatura zapłonu (°F): Not applicable
• Temperatura zapłonu (°C): Not applicable