Pomalidomide-PEG4-C2-NH2 is a high-purity E3 Ligase Ligand-Linker Conjugate specifically designed for the development of PROTAC (Proteolysis Targeting Chimera) molecules. This compound features pomalidomide, a potent thalidomide derivative recognized for its selective binding to the E3 ligase cereblon (CRBN), attached to a flexible PEG4 (polyethylene glycol) linker and terminated with a C2-amine (NH2) group. Such a configuration allows for efficient conjugation with various target protein ligands, facilitating the formation of heterobifunctional PROTACs. Designed to enable targeted protein degradation, Pomalidomide-PEG4-C2-NH2 acts as a bridging unit that recruits the E3 ligase complex to specific proteins of interest, inducing their ubiquitination and subsequent proteasomal degradation. This product is ideal for researchers engaged in chemical biology, drug discovery, and therapeutic development, offering a reliable and customizable scaffold for creating next-generation protein degraders targeting oncogenic, inflammatory, or other disease-related proteins.
Structure of 2225940-52-1
Quality Assurance
Worldwide Delivery
24/7 Customer Support
Category
E3 Ligase Ligand-Linker Conjugate
Molecular Formula
C23H32N4O8
Molecular Weight
492.52
* For research and manufacturing use only. Not for human or clinical use.
Size
Price
Stock
Quantity
--
$--
In stock
Looking for different specifications? Click to request a custom quote!
Pomalidomide-PEG4-C2-NH2 is a versatile E3 ligase ligand-linker conjugate widely used in the development of PROTACs (Proteolysis Targeting Chimeras). This bifunctional molecule harnesses pomalidomide, a high-affinity cereblon (CRBN) ligand, connected to a reactive amine terminus via a polyethylene glycol (PEG4) spacer and a two-carbon linker. Its rationally designed structure supports the modular assembly of heterobifunctional degraders for targeted protein degradation, facilitating innovative solutions in chemical biology and drug discovery.
Mechanism
The mechanism of Pomalidomide-PEG4-C2-NH2 relies on its ability to recruit the cereblon (CRBN) E3 ubiquitin ligase complex via the pomalidomide moiety. The conjugate's linker (PEG4-C2-NH2) provides both spacing and functional flexibility, enabling attachment to various ligands specific to proteins of interest. Once incorporated into a PROTAC molecule, this bifunctional agent simultaneously binds the target protein and CRBN, forming a ternary complex. This proximity-induced interaction promotes ubiquitination of the target protein, marking it for degradation by the ubiquitin-proteasome system.
Applications
Pomalidomide-PEG4-C2-NH2 finds broad applications in the synthesis of next-generation PROTACs and molecular glues for targeted protein degradation. Researchers leverage this ligand-linker conjugate to develop customized degraders against disease-relevant proteins, particularly in cancer, neurodegenerative diseases, and immunology. Its PEGylated linker enhances solubility and pharmacokinetic properties, proving valuable in both in vitro screening of PROTAC candidates and in vivo preclinical research. The reactive amine tail allows straightforward conjugation to diverse targeting ligands, supporting the rapid prototyping of novel E3 ligase-recruiting molecules tailored for therapeutic or mechanistic studies.
• Improved aqueous solubility and flexibility due to PEG4 linker, facilitating efficient PROTAC assembly.
• Amine-functionalized terminus enables versatile coupling strategies for streamlined CRBN E3 ligase-based PROTAC synthesis.
* 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.: 2225940-52-1
