Thalidomide-O-PEG4-Azide
This product is a heterobifunctional linker combining a thalidomide derivative, a PEG4 spacer, and a terminal azide. The thalidomide unit retains cereblon-binding activity, specifically enabling targeted recruitment in PROTAC and molecular glue design. The azide group supports copper-catalyzed (CuAAC) or copper-free (SPAAC) click chemistry with alkynes, while the PEG4 chain improves solubility and provides moderate spacing for flexible conjugation.
Key Features and Benefits
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Thalidomide Moiety: Binds cereblon E3 ligase for targeted protein degradation.
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Azide Group: Performs CuAAC or SPAAC click chemistry with alkyne partners.
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PEG4 Spacer: Enhances solubility and reduces steric hindrance.
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Dual Functionality: Combines biological targeting with modular click reactivity.
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High Purity: Produced to ≥95% purity for reliable performance.
Applications
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PROTAC Development: Links warheads to thalidomide for targeted protein degradation.
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Bioconjugation: Couples to alkyne-modified molecules via click chemistry.
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Probe Design: Builds bifunctional probes for mechanistic and imaging studies.
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Medicinal Chemistry: Serves as a versatile building block for cereblon-recruiting molecules.
Storage and Handling
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Storage: Store at –20 °C in a sealed, desiccated container.
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Handling: Use freshly prepared solutions; protect from light and moisture.
This product combines cereblon binding with azide click reactivity in a PEG4 framework, specifically offering a powerful tool for PROTAC design and advanced conjugation strategies.
AxisPharm offers 5000+ PEG Linkers with high purity. Different kinds of PEG Reagents may be available by custom synthesis.