Thalidomide-O-C5-acid is a specialized E3 Ligase Ligand-Linker Conjugate designed for advanced PROTAC (Proteolysis Targeting Chimera) drug development. This compound features a thalidomide-derived ligand that targets the cereblon (CRBN) E3 ubiquitin ligase, one of the most widely exploited ligases in targeted protein degradation strategies. By incorporating a C5-alkyl acid linker, Thalidomide-O-C5-acid provides a versatile functional group ideal for conjugation with various protein-targeting warheads, enabling the creation of bifunctional molecules that drive selective degradation of disease-relevant proteins. As a high-purity intermediate for medicinal chemistry, this product accelerates the development of novel PROTACs and related molecular glue degraders, supporting research in oncology, immunology, and neurodegenerative diseases. Thalidomide-O-C5-acid is an essential building block for scientists focused on harnessing the power of targeted protein degradation in drug discovery.
Structure of 2087490-48-8
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E3 Ligase Ligand-Linker Conjugate
Molecular Formula
C₁₉H₂₀N₂O₇
Molecular Weight
388.37
* For research and manufacturing use only. Not for human or clinical use.
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Thalidomide-O-C5-acid is a specialized E3 ligase ligand-linker conjugate designed for advanced applications in targeted protein degradation technologies, particularly PROTAC (Proteolysis Targeting Chimera) development. By leveraging the molecular framework of thalidomide, this compound serves as an essential building block to recruit the CRBN (Cereblon) E3 ubiquitin ligase within various bioconjugation and drug discovery platforms.
Mechanism
Thalidomide-O-C5-acid operates by binding to the Cereblon (CRBN) E3 ubiquitin ligase complex via its thalidomide moiety. The C5-alkyl acid linker introduces a functional handle for conjugation with diverse target protein ligands. When assembled as part of a PROTAC molecule, Thalidomide-O-C5-acid physically bridges the E3 ligase and the target protein, facilitating proximity-induced ubiquitination. This tagging marks the target for proteasomal degradation, enabling selective and efficient depletion of disease-related proteins from cells.
Applications
Thalidomide-O-C5-acid is widely utilized in the design, synthesis, and optimization of PROTACs, allowing researchers to target previously 'undruggable' proteins for degradation. Its modular structure supports the rapid generation of bifunctional molecules tailored for cancer, neurodegenerative, and autoimmune disease research. Furthermore, it serves as a versatile research tool in chemical biology, drug target validation, and next-generation therapeutics development—making it crucial for laboratories and pharmaceutical companies focused on protein-level drug discovery.
• Carboxylic acid-functionalized linker enables versatile conjugation to diverse warheads, facilitating custom PROTAC design.
• Optimized for efficient CRBN E3 ligase recruitment, supporting reliable and reproducible 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.: 2087490-48-8
