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 | |
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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. |