Mal-PEG1-Val-Cit-PAB-PNP
Mal-PEG1-Val-Cit-PAB-PNP is a high-purity cleavable PEG linker with a maleimide specifically for thiol-specific conjugation, a cathepsin B–cleavable Val-Cit dipeptide, and a para-aminobenzyl (PAB) self-immolative spacer linked to a para-nitrophenyl (PNP) carbonate for payload attachment. The short PEG1 spacer enhances solubility and flexibility, ensuring especially efficient bioconjugation in aqueous and organic systems while providing stability in circulation and controlled intracellular release for ADCs, targeted therapeutics, and diagnostic probes.
Key Features and Benefits
-
Maleimide Group: Selectively couples with thiols to form stable thioether bonds under mild conditions.
-
Val-Cit Cleavable Linker: Stable in systemic circulation and cleaved by cathepsin B inside target cells.
-
PAB Self-Immolative Spacer: Enables rapid and complete payload release after cleavage.
-
PNP Carbonate: Provides an activated site for efficient coupling to hydroxyl- or amine-containing payloads.
-
PEG1 Spacer: Improves solubility and minimizes steric hindrance for optimal reactivity.
Applications
-
Antibody–Drug Conjugates (ADCs): Link antibodies to cytotoxic drugs for targeted cancer therapy.
-
Peptide–Drug Conjugates: Enable enzyme-triggered, site-specific payload release.
-
Nanoparticle Functionalization: Add cleavable linkers for targeted delivery.
-
Prodrug Development: Incorporate linkers that activate in disease-specific environments.
-
Diagnostic Probe Development: Create targeted imaging agents with controlled release.
Storage and Handling
-
Storage: Store at –20 °C, dry, and protected from light.
-
Handling: Use anhydrous solvents such as DMF or DMSO; avoid moisture to preserve maleimide and PNP reactivity.
Mal-PEG1-Val-Cit-PAB-PNP integrates thiol-reactive maleimide chemistry, a cathepsin B–cleavable Val-Cit linker, a self-immolative PAB spacer, and a PNP carbonate payload attachment site in a short PEG1 framework for stable, targeted, and efficient bioconjugation.
AxisPharm offers 5000+ PEG Linkers with high purity. Different kinds of PEG Reagents may be available by custom synthesis.