CAS No.: 2376990-30-4 Cat No.: BP-100128 Purity: ≥95% by HPLC4.5
Thalidomide-O-amido-PEG2-C2-NH2 hydrochloride is a high-purity E3 Ligase Ligand-Linker Conjugate, primarily used in the design and synthesis of PROTACs (Proteolysis Targeting Chimeras). This compound features a thalidomide-based ligand, known for its selective binding to the cereblon (CRBN) E3 ubiquitin ligase, conjugated through a PEG2-C2 linker and terminated with an amine group (NH2), making it highly suitable for further functionalization and attachment to target warheads. As an essential building block in the development of next-generation protein degraders, Thalidomide-O-amido-PEG2-C2-NH2 hydrochloride enables researchers to create bifunctional molecules that harness the ubiquitin proteasome system (UPS) for targeted protein degradation—an emerging therapeutic modality in oncology, neurodegeneration, immune regulation, and beyond. Optimize your PROTAC research with this versatile ligand-linker intermediate, designed for efficient and selective E3 ligase recruitment and enhanced drug-like properties.
Structure of 2376990-30-4
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Category
E3 Ligase Ligand-Linker Conjugate
Molecular Formula
C₂₁H₂₇ClN₄O₈
Molecular Weight
498.91
* For research and manufacturing use only. Not for human or clinical use.
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Thalidomide-O-amido-PEG2-C2-NH2 hydrochloride is a specialized small-molecule reagent combining a thalidomide-based E3 ligase ligand with a polyethylene glycol (PEG2) linker and a terminal amine moiety. This conjugate is designed to facilitate the development and optimization of Proteolysis Targeting Chimeras (PROTACs), enabling targeted protein degradation by harnessing the cellular ubiquitin-proteasome system. Its structural features make it a valuable tool for drug discovery and research into targeted protein regulation.
Mechanism
This compound works as an E3 ligase ligand-linker conjugate. The thalidomide moiety selectively recruits the cereblon (CRBN) E3 ubiquitin ligase complex, an essential component for tagging target proteins for degradation. The PEG2-C2 linker offers an optimal spatial arrangement for connecting the E3 ligase ligand to a target protein ligand. The terminal NH2 group allows for versatile chemical conjugation, enabling the synthesis of bifunctional PROTAC molecules. Once the PROTAC is formed, it bridges the target protein and the E3 ligase, promoting polyubiquitination and subsequent proteasomal degradation of the target.
Applications
Thalidomide-O-amido-PEG2-C2-NH2 hydrochloride is widely employed in the design and synthesis of PROTACs for selective protein degradation. It serves as a modular intermediate for generating a variety of PROTACs by coupling with different ligands for target proteins, facilitating research in oncology, neurodegenerative diseases, and immunology. Additionally, it aids in structure-activity relationship (SAR) studies, linker optimization, and the creation of chemical biology probes. Its utility supports both academic and pharmaceutical research teams aiming to explore novel therapeutic modalities and target validation platforms.
• Amine-terminated PEG linker offers superior solubility and flexible conjugation options for custom PROTAC development.
• Optimized CRBN ligand ensures high binding affinity, enhancing selective protein degradation in targeted therapies.
* 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.: 2376990-30-4
Purity: ≥95% by HPLC
