904651

(S,R,S)-AHPC-PEG₃-azide

≥95%

• Sinônimo(s): (2S,4R)-1-((S)-14-azido-2-(tert-butyl)-4-oxo-6,9,12-trioxa-3-azatetradecanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide, Crosslinker−E3 Ligase ligand conjugate, Protein degrader building block for PROTAC^® research, Template for synthesis of targeted protein degrader, VH032 conjugate
• Fórmula empírica (Notação de Hill): C₃₀H₄₃N₇O₇S
• Número CAS: 1797406-80-4
• Peso molecular: 645.77
• Número MDL: MFCD31807299
• Código UNSPSC: 51171641
• NACRES: NA.22

Propriedades

• ligand: VH032
• Ensaio: ≥95%
• Formulário: solid or liquid
• adequação da reação: reaction type: click chemistry; reagent type: ligand-linker conjugate
• grupo funcional: azide
• temperatura de armazenamento: 2-8°C
• cadeia de caracteres 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=[N+]=[N-])=O)=O
• InChI: 1S/C30H43N7O7S/c1-20-26(45-19-33-20)22-7-5-21(6-8-22)16-32-28(40)24-15-23(38)17-37(24)29(41)27(30(2,3)4)35-25(39)18-44-14-13-43-12-11-42-10-9-34-36-31/h5-8,19,23-24,27,38H,9-18H2,1-4H3,(H,32,40)(H,35,39)/t23-,24+,27-/m1/s1
• chave InChI: MZOMHQGOVGODTD-ONBPZOJHSA-N

Descrição

Aplicação

Protein degrader building block (S,R,S)-AHPC-PEG₃-Azide 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 azide for click chemistry with a 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 azide group, parallel synthesis can be used to more quickly generate PROTAC libraries that feature variation in crosslinker length, composition, and E3 ligase ligand.

Automate your VHL-PEG based PROTACs with Synple Automated Synthesis Platform (SYNPLE-SC002)

Outras 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

Selective Small Molecule Induced Degradation of the BET Bromodomain Protein BRD4

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

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
• Ponto de fulgor (°F): Not applicable
• Ponto de fulgor (°C): Not applicable