2-(2,6-Dioxo-3-piperidinyl)-4-hydroxyisoindoline-1,3-dione
CAS No.: 5054-59-1
Cat No.: BP-200026
Purity: > 95 %
4.5 
2-(2,6-Dioxo-3-piperidinyl)-4-hydroxyisoindoline-1,3-dione is a versatile cereblon (CRBN) E3 ligase ligand commonly used in the design and synthesis of PROTACs (Proteolysis Targeting Chimeras) for targeted protein degradation. As a key thalidomide-based building block, this molecule enables efficient conjugation through its 4-hydroxy functional group, facilitating linker attachment during PROTAC development. It is valued for its high binding affinity to the CRBN E3 ubiquitin ligase and is instrumental in the discovery of small-molecule degraders for research into oncology, neurodegeneration, and other therapeutic areas. Category: E3 Ligase Ligand.
Structure of 5054-59-1
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* For research and manufacturing use only. Not for human or clinical use.
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- Comprehensive PROTAC Platform
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Background Introduction
2-(2,6-Dioxo-3-piperidinyl)-4-hydroxyisoindoline-1,3-dione is a structural analog of thalidomide, belonging to the family of IMiDs (immunomodulatory imide drugs). This compound contains a reactive hydroxy group at position 4 of the isoindoline core, representing a valuable scaffold for the design of Cereblon (CRBN)-recruiting E3 ligase ligands for targeted protein degradation strategies such as PROTACs (Proteolysis Targeting Chimeras) and molecular glues.
Mechanism
As a CRBN E3 ligase ligand, 2-(2,6-Dioxo-3-piperidinyl)-4-hydroxyisoindoline-1,3-dione selectively binds the Cereblon protein, a key substrate receptor within the CUL4-CRBN E3 ubiquitin ligase complex. When included in a bifunctional PROTAC molecule, it mediates the recruitment of the target protein—via a conjugated ligand—to the CRBN E3 ligase. This spatial proximity triggers ubiquitination of the target, marking it for selective degradation by the ubiquitin-proteasome system.
Applications
2-(2,6-Dioxo-3-piperidinyl)-4-hydroxyisoindoline-1,3-dione is a highly useful intermediate for constructing CRBN-based PROTACs and molecular glues. Its 4-hydroxy functional group allows facile chemical modification and linker attachment, supporting the development of custom degrader molecules. Common application areas include:
• Synthesis of CRBN E3 ligase-binding motifs for next-generation PROTACs• Structure-activity relationship (SAR) studies to optimize degrader efficacy in drug discovery
• Developing tool compounds for mechanistic studies of protein degradation
• Enabling academic and biotech research in targeted degradation platforms
• Consistent batch-to-batch reproducibility with complete QC documentation
• Supplied with COA, MSDS, and analytical data for traceability
• Reliable global shipping with stability-guaranteed packaging
• Dedicated technical support and optional custom synthesis service
• Demonstrates strong binding affinity to CRBN, VHL, or other E3 ligases
• Enables stable E3 ligase recruitment for targeted protein degradation
• High-affinity ligand for the CRBN E3 ligase ensures efficient target protein degradation in PROTAC development.
• Optimized chemical structure enables versatile conjugation, facilitating diverse PROTAC design and rapid SAR studies.
* Our calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
It is commonly abbreviated as: C1V1 = C2V2
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