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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
T15536 Hydroxy-PEG6-acid Hydroxy-PEG6-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.
T15878 m-PEG4-CH2COOH m-PEG4-CH2COOH 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.
T13998 1-(t-Boc-Aminooxy)-3-aminooxy-propane 1-(t-Boc-Aminooxy)-3-aminooxy-propane is an alkyl/ether-based PROTAC linker utilized in the synthesis of PROTACs[1].
T14485 Azidoethyl-SS-ethylazide Azidoethyl-SS-ethylazide is a cleavable linker employed for the synthesis of antibody-drug conjugates (ADCs)[1].
T18096 m-PEG-mal (MW 5000) m-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.
T16057 Methyltetrazine-PEG4-amine Methyltetrazine-PEG4-amine is a polyethylene glycol (PEG) derivative serving as a PROTAC linker for the synthesis of PROTACs[1].
T18563 Propargyl-O-C1-amido-PEG2-C2-NHS ester Propargyl-O-C1-amido-PEG2-C2-NHS ester is a non-cleavable 2-unit PEG linker employed in antibody-drug conjugation (ADC) to connect antibodies with drugs.
T16957 Sulfo DBCO-PEG4-amine Sulfo DBCO-PEG4-amine 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.
T14459 Azido-PEG5-CH2CO2-NHS Azido-PEG5-CH2CO2-NHS 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.
T15532 Hydroxy-PEG4-methylamine Hydroxy-PEG4-methylamine is a polyethylene glycol (PEG) derivative commonly employed as a linker in the synthesis of PROteolysis TArgeting Chimeras (PROTACs)[1].
T14795 Bromo-PEG3-azide Bromo-PEG3-azide 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.
T14623 Bis-Mal-Lysine-PEG4-acid Bis-Mal-Lysine-PEG4-acid is a PEG-based PROTAC linker utilized for PROTAC synthesis[1].
T14808 Bromo-PEG5-C2-acid Bromo-PEG5-C2-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.
T18814 Thalidomide-NH-PEG7 Thalidomide-NH-PEG7 is a synthesized conjugate of an E3 ligase ligand and linker designed for use in antibody-drug conjugates (ADCs). This compound can be coupled to a protein ligand via a linker to create PROTAC iRucaparib-AP6, an extremely selective degrader of PARP1[1].
T16981 TAMRA-Azide-PEG-biotin TAMRA-Azide-PEG-biotin 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.
T17132 Tos-PEG4-CH2COOH Tos-PEG4-CH2COOH 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.
T18374 N-(azide-PEG3)-N'-(Amine-C3-Amide-PEG4)-Cy5 N-(azide-PEG3)-N'-(Amine-C3-Amide-PEG4)-Cy5 is a polyethylene glycol (PEG)-based linker utilized in PROTAC synthesis [1].
T15057 DBCO-acid DBCO-acid is a cleavable ADC linker utilized in the synthesis of ADC linker DBCO-NHS ester and drug-linker conjugates DBCO-PEG-MMAE[1].
T18274 Mal-PEG12-NHS ester Mal-PEG12-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.
T15885 m-PEG4-sulfonic acid m-PEG4-sulfonic 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.
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