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Submit ReviewPhenyl-glutarimide 4'-piperazine is a piperazine-functionalized cereblon ligand that can be used for PROTAC® Degrader development. The compound can be used to develop PG-PROTACs that exhibit improved stability to hydrolysis and potency compared with PROTACs synthesized using IMiD (immunomodulatory imide drug) analogs.
Please contact us for SD files of our available Degrader Building Blocks.
PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.
This product is provided for use in onward chemistry. Suitable solvents can be used.
分子量 | 346.25 |
公式 | C15H19N3O2.2HCl |
储存 | Store at -20°C |
纯度 | ≥95% (HPLC) |
CAS Number | 2902651-89-0 |
InChI Key | DUZCAOXBUQOLHN-UHFFFAOYSA-N |
Smiles | O=C1CCC(C2=CC=C(N3CCNCC3)C=C2)C(N1)=O.Cl.Cl |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
参考文献是支持产品生物活性的出版物。
Min et al (2021) Phenyl-glutarimides: alternative cereblon binders for the design of PROTACs. Angew.Chem.Int.Ed. 60 26663 PMID: 34614283
Alcock et al (2022) Development of potent and selective Janus kinase 2/3 directing PG-PROTACs. ACS.Med.Chem.Lett. 13 475 PMID: 35300081
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关键词: Phenyl-glutarimide 4'-piperazine, Phenyl-glutarimide 4'-piperazine supplier, piperazine-functionalized, cereblon, ligand, phenyl-glutarimide, PROTAC, Degraders, building, blocks, targeted, protein, degradation, TPD, PG-PROTAC, pgprotac, protac-pg, Functionalized, E3, Ligase, Ligands, 7729, Tocris Bioscience
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Degraders (e.g. PROTACs) are bifunctional small molecules, that harness the Ubiquitin Proteasome System (UPS) to selectively degrade target proteins within cells. They consist of three covalently linked components: an E3 ubiquitin ligase ligand, a linker and a ligand for the target protein of interest. Authored in-house, this poster outlines the generation of a toolbox of building blocks for the development of Degraders. The characteristics and selection of each of these components are discussed. Presented at EFMC 2018, Ljubljana, Slovenia