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910554

Sigma-Aldrich

(S,R,S)-AHPC-PEG6-butyl CO2H

≥95%

Sinônimo(s):

(S)-3-((2S,4R)-4-Hydroxy-2-((4-(4-methylthiazol-5-yl)benzyl)carbamoyl)pyrrolidine-1-carbonyl)-2,2-dimethyl-5-oxo-7,10,13,16,19,22-hexaoxa-4-azanonacosan-29-oic acid, (S,R,S)-AHPC-2-2-2-2-2-2-6-Acid, Crosslinker−E3 ligase ligand conjugate, Protein degrader building block for PROTAC® research, Template for synthesis of targeted protein degrader, VH032 conjugate

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About This Item

Fórmula empírica (Notação de Hill):
C41H64N4O12S
Peso molecular:
837.03

ligand

VH032

Ensaio

≥95%

Formulário

(Liquid or Semi-Solid or Paste or Solid)

adequação da reação

reactivity: amine reactive
reagent type: ligand-linker conjugate

grupo funcional

carboxylic acid

temperatura de armazenamento

2-8°C

cadeia de caracteres SMILES

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)COCCOCCOCCOCCOCCOCCCCCCC(O)=O.Cl

Aplicação

Protein degrader building block (S,R,S)-AHPC-PEG6-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.

Informações legais

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

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Nº do produto
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Código de classe de armazenamento

12 - Non Combustible Liquids

Classe de risco de água (WGK)

WGK 3

Ponto de fulgor (°F)

Not applicable

Ponto de fulgor (°C)

Not applicable


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Ashton C Lai et al.
Angewandte Chemie (International ed. in English), 55(2), 807-810 (2015-11-26)
Proteolysis Targeting Chimera (PROTAC) technology is a rapidly emerging alternative therapeutic strategy with the potential to address many of the challenges currently faced in modern drug development programs. PROTAC technology employs small molecules that recruit target proteins for ubiquitination and

Artigos

Partial PROTACs are a collection of crosslinker-E3 ligand conjugates with a pendant functional group for covalent linkage to a target ligand.

Partial PROTACs are a collection of crosslinker-E3 ligand conjugates with a pendant functional group for covalent linkage to a target ligand.

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