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(S,R,S)-AHPC-piperazine-pyridine-alkyne-NH2 hydrochloride
产品别名
(S,R,S)-AHPC-piperazine-pyridine-alkyne-NH2 hydrochloride
Protein degrader building block for PROTAC research
(2S,4R)-1-((S)-2-(4-(4-(5-(3-Aminoprop-1-yn-1-yl)pyridin-2-yl)piperazin-1-yl)butanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide hydrochloride
Crosslinker-E3 Ligase ligand conjugate
VH032 conjugate
Template for synthesis of targeted protein degrader
结构式
基本信息
| Empirical Formula【经验(实验)分子式】 | C38H50N8O4S · xHCl |
| Molecular weight | 714.92 (free base basis) |
| Application【应用】 | Protein degrader building block (S,R,S)-AHPC-piperazine-pyridine-alkyne-NH2 hydrochloride 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 rigid linker, and a pendant amine for reactivity with a carboxylic acid 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 |
| form【形式】 | powder or crystals |
| storage temp.【储存温度】 | 2-8℃ |
| SMILES string | CC(N=CS1)=C1C2=CC=C(CNC([C@@H]3C[C@@H](O)CN3C([C@@H](NC(CCCN(CC4)CCN4C5=CC=C(C#CCN)C=N5)=O)C(C)(C)C)=O)=O)C=C2.Cl CC(N=CS1)=C1C2=CC=C(CNC([C@@H]3C[C@@H](O)CN3C([C@@H](NC(CCCN(CC4)CCN4C5=CC=C(C#CCN)C=N5)=O)C(C)(C)C)=O)=O)C=C2.Cl |
