BCN-PEG1-Val-Cit-PAB-OH
This product is a high-purity cleavable linker featuring a bicyclo[6.1.0]nonyne (BCN) group for rapid, copper-free strain-promoted azide–alkyne cycloaddition (SPAAC), a short PEG1 spacer for enhanced hydrophilicity, and a Val-Cit-PAB self-immolative unit for enzyme-triggered payload release. The Val-Cit dipeptide is specifically cleaved by cathepsin B in lysosomes, causing the PAB group to undergo 1,6-elimination and release the active payload. This design enables especially efficient, site-specific, and bioorthogonal conjugation for targeted drug delivery applications such as antibody–drug conjugates (ADCs).
Key Features and Benefits
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BCN Group – Supports fast, copper-free SPAAC click chemistry with azides for bioorthogonal conjugation.
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PEG1 Spacer – Improves aqueous solubility and reduces steric hindrance without significantly increasing linker length.
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Val-Cit-PAB Cleavable Linker – Cathepsin B–sensitive, enabling selective release of active payload in targeted cells.
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Self-Immolative Mechanism – PAB unit ensures clean and efficient payload liberation upon cleavage.
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High Purity – Supplied at >95% purity for reliable performance in demanding bioconjugation workflows.
Applications
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Antibody–drug conjugates (ADCs) and targeted therapeutics
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Bioorthogonal conjugation with azide-modified biomolecules
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Enzyme-cleavable linker design for drug delivery systems
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Development of multifunctional imaging and therapeutic agents
Storage and Handling
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Storage: Store at –20 °C, dry, and protected from light
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Handling: Use anhydrous solvents such as DMSO or DMF; avoid moisture to preserve reactivity
This product combines copper-free SPAAC click chemistry via BCN, a solubility-enhancing PEG1 spacer, and a cathepsin B–cleavable Val-Cit-PAB linker for especially precise, tumor-targeted payload release in ADC and drug delivery applications.
AxisPharm offers 5000+ PEG Linkers with high purity. Different kinds of PEG Reagents may be available by custom synthesis.
