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PROTAC Linker

The length and composition of the linker play critical roles in the physicochemical properties and bioactivity of PROTACs. While linker design has historically received limited attention, the PROTAC field is evolving rapidly and undergoing an important shift from synthetically tractable alkyl and polyethylene glycol to more sophisticated functional linkers. Equally important, linker-mediated binding cooperativity also represents a potential source of affinity for the POI for PROTACs based on weak affinity warheads. However, the current consensus is that the linker composition, and particularly its length and attachment point to the anchor/warhead, must be optimized for each ligand pair.

产品编号 产品名称
T18159 m-PEG17-NHS ester m-PEG17-NHS ester is a PEG-based linker for PROTACs which joins two essential ligands, crucial for forming PROTAC molecules. This linker enables selective protein degradation by leveraging the ubiquitin-proteasome system within cells.
T14799 Bromo-PEG3-CH2-Boc Bromo-PEG3-CH2-Boc is a PEG-based linker for PROTACs which joins two essential ligands, crucial for forming PROTAC molecules. This linker enables selective protein degradation by leveraging the ubiquitin-proteasome system within cells.
T15395 GMBS GMBS, a heterobifunctional cross-linker, possesses an N-hydroxysuccinimide (NHS) ester at one end and a maleimide group at the other. It is commonly used in bioconjugation to link amines and sulfhydryls [thiols], forming stable amide and thioether bonds, respectively, which are useful in creating protein and peptide conjugates.
T14699 BnO-PEG4-OH BnO-PEG4-OH is a PEG-based linker for PROTACs which joins two essential ligands, crucial for forming PROTAC molecules. This linker enables selective protein degradation by leveraging the ubiquitin-proteasome system within cells.
T18316 MC-Sq-Cit-PAB-Gefitinib MC-Sq-Cit-PAB-Gefitinib is a potent antitumor drug-linker conjugate for Antibody-Drug Conjugates (ADC), utilizing Gefitinib—an EGFR tyrosine kinase inhibitor—connected through the MC-Sq-Cit-PAB ADC linker.
T18005 HO-PEG-mal (MW 5000) HO-PEG-mal (MW 5000) is a PEG-based linker for PROTACs which joins two essential ligands, crucial for forming PROTAC molecules. This linker enables selective protein degradation by leveraging the ubiquitin-proteasome system within cells.
T18654 S-acetyl-PEG12-alcohol S-acetyl-PEG12-alcohol is a PEG-based linker for PROTACs which joins two essential ligands, crucial for forming PROTAC molecules. This linker enables selective protein degradation by leveraging the ubiquitin-proteasome system within cells.
T14482 Azido-PEG9-amine Azido-PEG9-amine, a non-cleavable 9-unit PEG ADC linker, is utilized in the synthesis of antibody-drug conjugates (ADCs)[1].
T18093 m-PEG-mal (MW 2000) m-PEG-mal (MW 2000) is a PEG-based linker for PROTACs which joins two essential ligands, crucial for forming PROTAC molecules. This linker enables selective protein degradation by leveraging the ubiquitin-proteasome system within cells.
T15951 Mal-amido-PEG2-NHS ester Mal-amido-PEG2-NHS ester is a noncleavable linker for antibody-drug conjugates (ADCs) that consists of a maleimide group and an NHS ester. The NHS ester allows for the labeling of protein primary amines (-NH2), amine-modified oligonucleotides, and other amine-containing molecules[1][2].
T18778 TCO-PEG6-NHS ester TCO-PEG6-NHS ester is a PEG-based linker for PROTACs which joins two essential ligands, crucial for forming PROTAC molecules. This linker enables selective protein degradation by leveraging the ubiquitin-proteasome system within cells.
T17675 Boc-NH-PEG24-CH2CH2COOH Boc-NH-PEG24-CH2CH2COOH is a polyethylene glycol (PEG)-based linker for PROTAC (Proteolysis-Targeting Chimeras) synthesis[1].
T15911 m-PEG7-CH2-OH m-PEG7-CH2-OH is a PEG-based linker for PROTACs which joins two essential ligands, crucial for forming PROTAC molecules. This linker enables selective protein degradation by leveraging the ubiquitin-proteasome system within cells.
T18644 PTAD-PEG4-N3 PTAD-PEG4-N3 is a cleavable four-unit polyethylene glycol (PEG) antibody-drug conjugate (ADC) linker, utilized in ADC synthesis[1].
T15538 Hydroxy-PEG6-CH2-Boc Hydroxy-PEG6-CH2-Boc is a PEG-based linker for PROTACs which joins two essential ligands, crucial for forming PROTAC molecules. This linker enables selective protein degradation by leveraging the ubiquitin-proteasome system within cells.
T14798 Bromo-PEG3-C2-phosphonic acid Bromo-PEG3-C2-phosphonic acid is a polyethylene glycol (PEG) derivative serving as a linker in the synthesis of proteolysis targeting chimeras (PROTACs)[1].
T18572 Propargyl-PEG14-acid Propargyl-PEG14-acid is a PEG-based linker for PROTACs which joins two essential ligands, crucial for forming PROTAC molecules. This linker enables selective protein degradation by leveraging the ubiquitin-proteasome system within cells.
T18655 S-acetyl-PEG16-alcohol S-acetyl-PEG16-alcohol is a PEG-based linker for PROTACs which joins two essential ligands, crucial for forming PROTAC molecules. This linker enables selective protein degradation by leveraging the ubiquitin-proteasome system within cells.
T18424 N-(m-PEG4)-N'-(azide-PEG4)-Cy3 N-(m-PEG4)-N'-(azide-PEG4)-Cy3 is a polyethylene glycol (PEG)-derived linker, specifically designed for the synthesis of proteolysis targeting chimeras (PROTACs)[1].
T18439 N-(m-PEG9)-N'-(propargyl-PEG8)-Cy5 N-(m-PEG9)-N'-(propargyl-PEG8)-Cy5 is a polyethylene glycol (PEG)-based PROTAC linker, specifically designed to aid in the synthesis of PROTACs[1].
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