901511

(S,R,S)-AHPC-PEG₃-NH₂ hydrochloride

≥95%

• Sinónimos: (2S,4R)-1-((S)-14-Amino-2-(tert-butyl)-4-oxo-6,9,12-trioxa-3-azatetradecanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide hydrochloride, Crosslinker–E3 Ligase ligand conjugate, Protein degrader building block for PROTAC^® research, Template for synthesis of targeted protein degrader, VH032 conjugate
• Fórmula empírica (notación de Hill): C₃₀H₄₅N₅O₇S · xHCl
• Número de CAS: 2097971-11-2
• Peso molecular: 619.77 (free base basis)
• Número MDL: MFCD31656714
• Código UNSPSC: 12352101
• NACRES: NA.22

Propiedades

• ligand: VH032
• Nivel de calidad: 100
• Ensayo: ≥95%
• Formulario: powder or crystals
• idoneidad de la reacción: reactivity: carboxyl reactive; reagent type: ligand-linker conjugate
• grupo funcional: amine
• temp. de almacenamiento: 2-8°C
• cadena SMILES: O=C(NCC1=CC=C(C2=C(C)N=CS2)C=C1)[C@H](C[C@@H](O)C3)N3C([C@H](C(C)(C)C)NC(COCCOCCOCCN)=O)=O.Cl
• Clave InChI: ZOYHUTRHKHRRPK-QVRKWNSCSA-N

Descripción

Aplicación

Protein degrader builiding block (S,R,S)-AHPC-PEG₃-NH₂ (HCl salt) 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 and a PEGylated crosslinker with pendant amine for reactivity with a carboxyl group 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 amine, parallel synthesis can be used to more quickly generate PROTAC libraries that feature variation in crosslinker length, composition, and E3 ligase ligand.

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Otras notas

Technology Spotlight: Degrader Building Blocks for Targeted Protein Degradation

Portal: Building PROTAC^® Degraders for Targeted Protein Degradation

Impact of Target Warhead and Linkage Vector on Inducing Protein Degradation: Comparison of Bromodomain and Extra-Terminal (BET) Degraders Derived from Triazolodiazepine (JQ1) and Tetrahydroquinoline (I-BET726) BET Inhibitor Scaffolds

Degradation of the BAF Complex Factor BRD9 by Heterobifunctional Ligands

Assessing Different E3 Ligases for Small Molecule Induced Protein Ubiquitination and Degradation

Targeted Protein Degradation by Small Molecules

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

Información de seguridad

• Pictogramas: GHS07
• Palabra de señalización: Warning
• Frases de peligro: H302,H315,H319
• Consejos de prudencia: P264 - P280 - P301 + P312 - P302 + P352 - P305 + P351 + P338 - P332 + P313
• Clasificaciones de peligro: Acute Tox. 4 Oral - Eye Irrit. 2 - Skin Irrit. 2
• Código de clase de almacenamiento: 11 - Combustible Solids
• Clase de riesgo para el agua (WGK): WGK 3
• Punto de inflamabilidad (°F): Not applicable
• Punto de inflamabilidad (°C): Not applicable