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产品别名
(S,R,S)-AHPC-PEG1-Alkyne
CrosslinkerE3 Ligase ligand conjugate
Protein degrader building block for PROTAC research
VH032 conjugate
Template for synthesis of targeted protein degrader
(2S,4R)-1-((S)-3,3-Dimethyl-2-(3-(prop-2-yn-1-yloxy)propanamido)butanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide
结构式
基本信息
| Empirical Formula【经验(实验)分子式】 | C28H36N4O5S |
| Molecular weight | 540.67 |
| Application【应用】 | Protein degrader builiding block (S,R,S)-AHPC-PEG1-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. |
| Other Notes【其他说明】 | Technology Spotlight: Degrader Building Blocks for Targeted Protein Degradation Portal: 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 |
| Legal Information【法律信息】 | PROTAC is a registered trademark of Arvinas Operations, Inc., and is used under license |
产品性质
| Quality Level【质量水平】 | 100 |
| Assay【测定】 | ≥95% |
| form【形式】 | powder or crystals |
| reaction suitability | reaction type: click chemistry |
| storage temp.【储存温度】 | 2-8℃ |
| SMILES string | 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(CCOCC#C)=O)=O 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(CCOCC#C)=O)=O |
安全信息
| Storage Class Code【储存分类代码】 | 13 - Non Combustible Solids |
| WGK | WGK 3 |
