929352

(S,R,S)-AHPC-di-trimethylamide-dioxodisulfide-carbonate ester

• Sinônimo(s): S-(1-(((((3R,5S)-1-((S)-2-((tert-butoxycarbonyl)amino)-3,3-dimethylbutanoyl)-5-((4-(4-methylthiazol-5-yl)benzyl)carbamoyl)pyrrolidin-3-yl)oxy)carbonyl)oxy)-2-methylpropan-2-yl) methanesulfonothioate
• Fórmula empírica (Notação de Hill): C₃₃H₄₈N₄O₉S₃
• Número CAS: 2417370-08-0
• Peso molecular: 740.95
• Código UNSPSC: 12352108
• NACRES: NA.21

Propriedades

• ligand: VH032
• Ensaio: ≥95%
• forma: powder
• grupo funcional: disulfide
• temperatura de armazenamento: 2-8°C
• cadeia de caracteres SMILES: CC(C)(C)OC(N[C@@H](C(C)(C)C)C(N1[C@@H](C[C@H](C1)OC(OCC(C)(C)SS(C)(=O)=O)=O)C(NCC2=CC=C(C3=C(C)N=CS3)C=C2)=O)=O)=O

Descrição

Aplicação

Protein degrader building block (S,R,S)-AHPC-di-trimethylamide-dioxodisulfide-carbonate ester enables the synthesis of molecules for degradation of proteins and PROTAC^® (proteolysis-targeting chimeras) research. This conjugate contains a von Hippel-Lindau (VHL)-recruiting ligand and a pendant disulfide, linked via a carbonate group. The pendant disulfide allows for targeted degradation of antibodies. 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, 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

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Outras notas

Targeted Protein Degradation by Small Molecules

Antibody Conjugation of a Chimeric BET Degrader Enables in vivo Activity

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

Informações legais

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

Informações de segurança

• Código de classe de armazenamento: 11 - Combustible Solids
• Classe de risco de água (WGK): WGK 3