产品说明
应用
Protein degrader building block Pomalidomide-piperazine-piperidine-4-carboxamide hydrochloride enables the synthesis of molecules for targeted protein degradation and PROTAC® (proteolysis-targeting chimeras) research. This conjugate contains a Cereblon (CRBN) 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 degrader, many analogs are prepared to screen for optimal target degradation. When used with other protein degrader building blocks with a terminal amine, parallel synthesis can be used to more quickly generate degrader libraries that feature variation in crosslinker length, composition, and E3 ligase ligand.
Technology Spotlight: Degrader Building Blocks for Targeted Protein Degradation
Protein Degrader Building Blocks
其他说明
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
法律信息
PROTAC is a registered trademark of Arvinas Operations, Inc., and is used under license
基本信息
经验(实验)分子式 | C23H27N5O5 · xHCl |
分子量 | 453.49 (free base basis) |
产品性质
质量水平 | 100 |
储存温度 | 2-8℃ |
SMILES string | O=C1C(N2C(C(C=CC=C3N4CCN(C(C5CCNCC5)=O)CC4)=C3C2=O)=O)CCC(N1)=O.Cl |
Sigma-Aldrich