Thalidomide-4-NH-PEG1-NH-Boc is an advanced E3 ligase ligand engineered for PROTAC (Proteolysis Targeting Chimera) and molecular glue research applications. This derivative features a PEG1 linker and an N-Boc protecting group at the 4-amino position, allowing flexible further modification and conjugation. Thalidomide scaffolds are widely used as cereblon (CRBN) recruiting elements in targeted protein degradation strategies, facilitating the development of next-generation therapeutics. Thalidomide-4-NH-PEG1-NH-Boc serves as a versatile building block for designing and optimizing CRBN-based degraders in PROTAC drug discovery and chemical biology studies.
Structure of 2154342-17-1
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Category
Ligand for E3 Ligase
Molecular Formula
C22H28N4O7
Molecular Weight
460.48
* For research and manufacturing use only. Not for human or clinical use.
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Thalidomide and its structural analogs serve as quintessential Cereblon (CRBN) E3 ligase ligands, enabling targeted protein degradation (TPD) through the PROTAC platform. Thalidomide-4-NH-PEG1-NH-Boc is a rationally designed derivative featuring a PEGylated (polyethylene glycol unit) linker and a Boc-protected amine. This building block improves the hydrophilicity and solubility of resultant PROTAC molecules, while providing a versatile amine handle for further chemical modifications.
Mechanism
Thalidomide-4-NH-PEG1-NH-Boc utilizes its thalidomide core to engage the CRBN component of the CUL4-CRBN E3 ligase complex. The PEG1 spacer increases molecular flexibility and modulates physicochemical properties, enhancing the pharmacokinetic profile of the final degrader molecules. The terminal Boc-protected amine enables orthogonal deprotection and site-specific conjugation to target protein ligands, optimizing the spatial arrangement essential for efficient ubiquitination and proteasomal degradation of the target protein.
Applications
This compound is an essential intermediate in the development of CRBN-based PROTACs and molecular glue degraders. Its combination of PEG linkers and protected amine functionality is ideal for constructing diverse libraries of bifunctional degraders in drug discovery and chemical biology. Key application areas include:
• Synthesis of CRBN-targeting PROTACs with improved aqueous solubility and cell permeability
• Development of customized protein degraders in medicinal chemistry and target validation projects
• Late-stage functionalization for SAR studies and linker optimization
• Assembly of molecular glue candidates for translational and academic research
• High-purity compound verified by HPLC, NMR, and LC-MS
• 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
• Features a protected PEGylated linker that enhances solubility and offers versatile conjugation options for PROTAC synthesis.
• Optimized for efficient recruitment of cereblon (CRBN) E3 ligase, empowering targeted protein degradation research.
* 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
CAS No.: 2154342-17-1
