CAS No.: 2245697-88-3 Cat No.: BP-100059 Purity: ≥98%4.5
Thalidomide-linker 4 is an advanced E3 ligase ligand-linker conjugate specifically designed for use in the development of PROTAC (Proteolysis Targeting Chimera) molecules. As a thalidomide-derived compound, it efficiently recruits the cereblon (CRBN) E3 ubiquitin ligase, enabling the targeted degradation of disease-related proteins. This conjugate features a pre-attached linker, streamlining the synthesis of bifunctional PROTACs and molecular glues. Thalidomide-linker 4 is ideal for researchers focusing on drug discovery against undruggable targets, as it promotes selective protein degradation through the ubiquitin-proteasome system. It is widely used in cancer research, neuroscience, and other therapeutic areas seeking next-generation treatment strategies. As part of the E3 Ligase Ligand-Linker Conjugate category, Thalidomide-linker 4 offers optimal reactivity, high purity, and reliable performance for medicinal chemistry and chemical biology applications.
Structure of 2245697-88-3
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Category
E3 Ligase Ligand-Linker Conjugate
Molecular Formula
C19H23N3O5.HCl
Molecular Weight
409.86
* For research and manufacturing use only. Not for human or clinical use.
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Thalidomide-linker 4 is a specialized E3 ligase ligand-linker conjugate designed to facilitate targeted protein degradation via PROTAC (Proteolysis Targeting Chimera) technology. As a derivative of thalidomide, this compound harnesses cereblon (CRBN) as the E3 ligase recruiter, making it a popular choice for constructing effective and selective PROTAC molecules. The addition of a functionalized linker provides a versatile handle for conjugation to various target protein ligands, enabling rapid prototyping and optimization of bifunctional molecules for research and development.
Mechanism
Thalidomide-linker 4 operates through a bifunctional mechanism central to PROTAC technology. The thalidomide-based moiety binds specifically to the CRBN E3 ubiquitin ligase, while the customizable linker serves as a bridge to conjugate the molecule to a ligand that binds the protein of interest. Once the PROTAC molecule is formed and introduced into a cellular system, it simultaneously brings the CRBN E3 ligase in close proximity to the target protein. This induced proximity triggers the ubiquitination and subsequent proteasomal degradation of the targeted protein, enabling selective and efficient knockdown at the post-translational level.
Applications
Thalidomide-linker 4 is widely used in the development and optimization of PROTACs for both basic research and drug discovery. Its applications include: (1) Creation of targeted protein degraders for oncology, immunology, and neurodegenerative disease research; (2) Investigation of degradation mechanisms and E3 ligase selectivity in cellular environments; (3) Development of novel therapeutic candidates by enabling rapid generation of bifunctional molecules; and (4) Structure-activity relationship (SAR) studies to fine-tune linker length, stability, and selectivity of PROTAC compounds. This versatile intermediate is ideal for scientists seeking to accelerate the design and synthesis of next-generation protein degraders.
• Thalidomide-linker 4 delivers reliable CRBN E3 ligase recruitment, enabling targeted protein degradation in PROTAC applications.
• Versatile linker structure supports seamless conjugation with diverse warheads, optimizing PROTAC design flexibility.
* 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.: 2245697-88-3
Purity: ≥98%
