The Role of Azido-PEG2-Alcohol in PROTAC Drug Discovery
The landscape of pharmaceutical research is constantly evolving, with innovative therapeutic modalities emerging to tackle previously intractable diseases. Among the most exciting advancements is the development of Proteolysis Targeting Chimeras (PROTACs), a revolutionary class of drugs that harness the cell's own degradation machinery to eliminate disease-causing proteins.
At the heart of a PROTAC molecule lies a linker that connects a protein-binding ligand to an E3 ligase-binding ligand. The chemical properties of this linker are critical for the PROTAC's efficacy, influencing its shape, solubility, stability, and ability to recruit the target protein and E3 ligase effectively. Among the diverse linker chemistries being explored, polyethylene glycol (PEG) derivatives, particularly those functionalized with azide groups, have gained significant traction. This is where 2-(2-Azidoethoxy)ethanol (CAS 139115-90-5) plays a pivotal role.
Why Azido-PEG2-Alcohol is Key for PROTACs
2-(2-Azidoethoxy)ethanol, often referred to as Azido-PEG2-alcohol, possesses a unique structure that makes it an ideal building block for PROTAC linkers:
- PEG Spacer: The short polyethylene glycol (PEG) chain provides hydrophilicity, improving the solubility and pharmacokinetic properties of the resulting PROTAC molecule. This can be crucial for oral bioavailability and systemic distribution.
- Azide Functional Group: The terminal azide group (N3) is a highly versatile functional handle. It is a key participant in 'click chemistry' reactions, particularly the copper(I)-catalyzed azide-alkyne cycloaddition (CuAAC) and strain-promoted azide-alkyne cycloaddition (SPAAC). These reactions are highly efficient, specific, and occur under mild conditions, making them perfect for conjugating complex biomolecules without damaging sensitive functional groups.
- Hydroxyl Group: The terminal hydroxyl group (-OH) allows for further chemical modifications. It can be readily functionalized with other reactive groups or used to attach one of the PROTAC ligands, offering flexibility in linker design.
The combination of these features in 2-(2-Azidoethoxy)ethanol (C4H9N3O2, MW 131.13) allows medicinal chemists to design PROTACs with tailored linker lengths and compositions, optimizing their interaction with target proteins and E3 ligases. As researchers push the boundaries of targeted protein degradation, the demand for high-quality intermediates like this continues to grow.
Procuring 2-(2-Azidoethoxy)ethanol for Your Research
Given its critical role in cutting-edge drug discovery, sourcing reliable and high-purity 2-(2-Azidoethoxy)ethanol is essential. When looking to buy this intermediate, consider the following:
- Purity: High purity (e.g., ≥97% or ≥98%) is paramount to ensure the success of click chemistry reactions and the integrity of your PROTAC constructs.
- Supplier Reliability: Partnering with a reputable manufacturer and supplier, especially one with a strong presence in producing chemical intermediates for the pharmaceutical industry, is key.
- Technical Specifications: Ensure the supplier provides clear technical data, including CAS number (139115-90-5), molecular formula, and molecular weight.
- Scalability: For projects progressing to later stages, the ability to scale up supply from research quantities to bulk is a significant advantage.
NINGBO INNO PHARMCHEM CO.,LTD. as Your PROTAC Linker Supplier
NINGBO INNO PHARMCHEM CO.,LTD. is a premier chemical manufacturer and supplier dedicated to providing the high-quality intermediates necessary for advanced pharmaceutical research. Our 2-(2-Azidoethoxy)ethanol (CAS 139115-90-5) is produced under stringent quality controls, ensuring the high purity required for PROTAC synthesis and other click chemistry applications. We offer competitive pricing and reliable delivery, making us an ideal partner for drug discovery organizations worldwide. If you are developing PROTACs or exploring other click chemistry-based applications, we encourage you to inquire about our Azido-PEG2-alcohol and discover how our commitment to quality and service can support your innovative projects.
Perspectives & Insights
Alpha Spark Labs
“At the heart of a PROTAC molecule lies a linker that connects a protein-binding ligand to an E3 ligase-binding ligand.”
Future Pioneer 88
“The chemical properties of this linker are critical for the PROTAC's efficacy, influencing its shape, solubility, stability, and ability to recruit the target protein and E3 ligase effectively.”
Core Explorer Pro
“Among the diverse linker chemistries being explored, polyethylene glycol (PEG) derivatives, particularly those functionalized with azide groups, have gained significant traction.”