910600

(S,R,S)-AHPC-PEG₂-butyl CO₂H

≥95%

• 동의어(들): (S,R,S)-AHPC-2-2-6-acid, 7-(2-(2-(((S)-1-((2S,4R)-4-Hydroxy-2-((4-(4-methylthiazol-5-yl)benzyl)carbamoyl)pyrrolidin-1-yl)-3,3-dimethyl-1-oxobutan-2-yl)amino)-2-oxoethoxy)ethoxy)heptanoic acid, Crosslinker−E3 ligase ligand conjugate, Protein degrader building block for PROTAC^® research, Template for synthesis of targeted protein degrader, VH032 conjugate
• 실험식(Hill 표기법): C₃₃H₄₈N₄O₈S
• Molecular Weight: 660.82
• UNSPSC 코드: 12352200
• NACRES: NA.22

속성

• ligand: VH032
• 분석: ≥95%
• 양식: crystals
• 반응 적합성: reactivity: amine reactive; reagent type: ligand-linker conjugate
• 작용기: carboxylic acid
• 저장 온도: 2-8°C
• SMILES string: O=C(N[C@H](C(N1[C@H](C(NCC2=CC=C(C3=C(C)N=CS3)C=C2)=O)C[C@@H](O)C1)=O)C(C)(C)C)COCCOCCCCCCC(O)=O.Cl

설명

애플리케이션

Protein degrader builiding block (S,R,S)-AHPC-PEG₂-butyl CO₂H 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 linker with both hydrophobic and hydrophilic moieties, and a pendant carboxylic acid for reactivity with an amine 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 carboxyl group, parallel synthesis can be used to more quickly generate PROTAC libraries that feature variation in crosslinker length, composition, and E3 ligase ligand.

기타 정보

Technology Spotlight: Partial PROTACs for Targeted Protein Degradation

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

법적 정보

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

안전성 정보

• Storage Class Code: 10 - Combustible liquids
• WGK: WGK 3
• Flash Point (°F): Not applicable
• Flash Point (°C): Not applicable