Pomalidomide-PEG4-azide is a high-purity E3 Ligase Ligand-Linker Conjugate designed for advanced research in PROTAC (Proteolysis Targeting Chimera) drug development. This specialized molecule features Pomalidomide—a potent cereblon (CRBN) E3 ubiquitin ligase ligand—covalently linked to a PEG4 (polyethylene glycol) spacer terminated with an azide functional group. The azide moiety enables efficient 'click chemistry' for modular conjugation with a variety of targeting ligands, empowering rapid synthesis of novel bifunctional PROTACs.
As a critical starting material in targeted protein degradation research, Pomalidomide-PEG4-azide facilitates the recruitment of CRBN E3 ligase, leading to selective ubiquitination and proteasomal degradation of disease-associated proteins. This conjugate is ideal for medicinal chemistry projects targeting cancer, neurodegenerative disorders, and other conditions where PROTAC technology offers significant therapeutic promise. All batches are synthesized to rigorous quality standards, ensuring reliable performance in drug discovery, library development, and chemical biology applications.
Structure of 2271036-47-4
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Category
E3 Ligase Ligand-Linker Conjugate
Molecular Formula
C₂₃H₃₀N₆O₈
Molecular Weight
518.52
* For research and manufacturing use only. Not for human or clinical use.
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Pomalidomide-PEG4-azide is a versatile PROTAC building block that combines the immunomodulatory drug pomalidomide—an E3 ligase ligand—with a PEG4 linker terminated by an azide functional group. This design enables rapid and efficient conjugation via click chemistry, making it a valuable tool for developing customized PROTAC molecules and molecular glues for targeted protein degradation.
Mechanism
The mechanism of Pomalidomide-PEG4-azide centers on its ability to recruit the cereblon (CRBN) E3 ubiquitin ligase complex through the pomalidomide moiety. When linked to a specific target protein ligand via the PEG4-azide handle, it forms a bifunctional molecule capable of simultaneously binding CRBN and the target protein. This proximity induces ubiquitination of the target protein, leading to its subsequent degradation by the proteasome. The azide group on the linker enables user-friendly click chemistry (e.g., CuAAC), simplifying the construction of diverse PROTAC molecules.
Applications
Pomalidomide-PEG4-azide is widely used in the synthesis of next-generation PROTACs and other heterobifunctional degraders. Its key applications include developing custom PROTACs for targeted protein degradation research, constructing protein degradation tools for drug discovery, and creating chemical probes to study protein function in cellular systems. The azide functionality also allows site-specific labelling, bioconjugation, and expansion into various click chemistry-based applications. This conjugate is highly valuable for oncology research, neurodegenerative disorder studies, and functional genomics screening.
• PEG4-azide functional group enables versatile click chemistry conjugation for streamlined PROTAC assembly.
• Pomalidomide moiety ensures high specificity and affinity for CRBN E3 ligase, supporting efficient protein degradation.
* 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.: 2271036-47-4
