901534

(S,R,S)-AHPC-C₆-CO₂H hydrochloride

• 别名: 7-(((S)-1-((2S,4R)-4-Hydroxy-2-((4-(4-methylthiazol-5-yl)benzyl)carbamoyl)pyrrolidin-1-yl)-3,3-dimethyl-1-oxobutan-2-yl)amino)heptanoic acid, Crosslinker−E3 Ligase ligand conjugate, Protein degrader building block for PROTAC^® research, Template for synthesis of targeted protein degrader, VH032 conjugate
• 经验公式（希尔记法）: C₂₉H₄₂N₄O₅S · xHCl
• 分子量: 558.73 (free base basis)
• MDL號碼: MFCD32062444
• 分類程式碼代碼: 12352101
• NACRES: NA.22

属性

• ligand: VH032
• 品質等級: 100
• 化驗: ≥95%
• 形狀: powder
• 反應適用性: reactivity: amine reactive; reagent type: ligand-linker conjugate
• 官能基: carboxylic acid
• 儲存溫度: 2-8°C
• SMILES 字串: 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)NCCCCCCC(O)=O)=O.Cl
• InChI: 1S/C29H42N4O5S.ClH/c1-19-25(39-18-32-19)21-12-10-20(11-13-21)16-31-27(37)23-15-22(34)17-33(23)28(38)26(29(2,3)4)30-14-8-6-5-7-9-24(35)36;/h10-13,18,22-23,26,30,34H,5-9,14-17H2,1-4H3,(H,31,37)(H,35,36);1H/t22-,23+,26-;/m1./s1
• InChI 密鑰: PWGKDPPFSKFPCC-VIXMLYKZSA-N

说明

應用

Protein degrader builiding block (S,R,S)-AHPC-C₆-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 and an alkyl-chain crosslinker with 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.

其他說明

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

法律資訊

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

安全信息

• 儲存類別代碼: 11 - Combustible Solids
• 水污染物質分類（WGK）: WGK 3
• 閃點（°F）: Not applicable
• 閃點（°C）: Not applicable