Phenyl-glutarimide 4'-oxyacetic acid

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Description: Functionalized cereblon ligand for PROTAC development
Chemical Name: 2-(4-(2,6-Dioxopiperidin-3-yl)phenoxy)acetic acid
Purity: ≥95% (HPLC)
Datasheet
Citations
Reviews
Literature (1)

Biological Activity

Phenyl-glutarimide 4'-oxyacetic acid is a carboxylic acid-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.

Usage Guidelines

This product is provided for use in onward chemistry. Suitable solvents can be used.

Technical Data

M. Wt 263.25
Formula C13H13NO5
Storage Store at -20°C
Purity ≥95% (HPLC)
CAS Number 2782024-58-0
InChI Key AJINEEJVZAYBCQ-UHFFFAOYSA-N
Smiles O=C(N1)CCC(C2=CC=C(C=C2)OCC(O)=O)C1=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Product Datasheets

Certificate of Analysis / Product Datasheet
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References

References are publications that support the biological activity of the product.

Min et al (2021) Phenyl-glutarimides: alternative cereblon binders for the design of PROTACs. Angew.Chem.Int.Ed. 60 26663 PMID: 34614283


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Literature in this Area

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Targeted Protein Degradation Poster

Targeted Protein Degradation Poster

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