cIAP1 Ligand-Linker Conjugates 3 are specialized chemical intermediates designed for use in the development of PROTACs (Proteolysis Targeting Chimeras). Classified as E3 Ligase Ligand-Linker Conjugates, these compounds comprise a selective ligand for the cellular inhibitor of apoptosis protein 1 (cIAP1) E3 ubiquitin ligase tethered to a functionalized linker. In PROTAC technology, cIAP1 Ligand-Linker Conjugates serve as critical building blocks that recruit cIAP1 to a target protein, promoting its ubiquitination and subsequent degradation via the proteasome pathway. By leveraging the ubiquitin-proteasome system, researchers can design highly selective and potent degraders of disease-associated proteins. cIAP1-based PROTACs are actively explored for their potential applications in oncology, neurodegenerative diseases, and immunology. These conjugates offer versatility for synthesizing PROTAC molecules targeting a wide array of intracellular proteins, accelerating drug discovery, and enabling novel therapeutic strategies.
Structure of 2222354-20-1
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Category
E3 Ligase Ligand-Linker Conjugate
Molecular Formula
C39H56N4O11S
Molecular Weight
788.95
* For research and manufacturing use only. Not for human or clinical use.
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cIAP1 Ligand-Linker Conjugates 3 are cutting-edge chemical tools specifically designed for targeted protein degradation applications. Leveraging the ubiquitin-proteasome system, these conjugates incorporate an optimized ligand that selectively binds to the cellular inhibitor of apoptosis protein 1 (cIAP1) E3 ligase, coupled with a chemically tailored linker to facilitate efficient conjugation with target protein ligands. These conjugates are highly valuable in PROTAC and related targeted protein degradation research, enabling scientists to explore novel therapeutic strategies for modulating undruggable proteins.
Mechanism
The cIAP1 Ligand-Linker Conjugates 3 function by recruiting the cIAP1 E3 ubiquitin ligase to the protein of interest when incorporated into a PROTAC (Proteolysis Targeting Chimera) molecule. The cIAP1-binding ligand ensures high affinity and specificity for the E3 ligase, while the linker provides optimal flexibility and spatial arrangement to bring the E3 ligase and the target protein into close proximity. Once the PROTAC molecule bridges the cIAP1 E3 ligase and the target protein, cIAP1 mediates ubiquitination of the target, which tags it for rapid proteasomal degradation, resulting in selective and potent depletion of disease-related proteins at the cellular level.
Applications
cIAP1 Ligand-Linker Conjugates 3 are primarily used in the synthesis of next-generation PROTACs for both in vitro and in vivo studies. Their applications include the development of novel therapeutic candidates for cancer, neurodegenerative diseases, and other conditions involving pathogenic proteins. Additionally, these conjugates are instrumental in basic research focused on protein homeostasis, targeted protein degradation mechanisms, and chemical biology investigations. They enable the creation of degrader molecules tailored to specific targets, expanding the therapeutic landscape beyond traditional inhibition strategies and opening doors to drug discovery against previously 'undruggable' proteins.
• Specifically designed for seamless integration into cIAP1-targeting PROTACs, enabling efficient ubiquitination and degradation of disease-related proteins.
• Customizable linker architecture ensures optimal proximity and flexibility, maximizing PROTAC potency and cellular permeability for advanced drug discovery applications.
* 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.: 2222354-20-1
