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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T18212 | m-PEG6-Ms | m-PEG6-Ms 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. |
T16171 | N-(Amino-PEG3)-N-bis(PEG3-Boc) | N-(Amino-PEG3)-N-bis(PEG3-Boc) is a polyethylene glycol-based linker utilized in the synthesis of proteolysis targeting chimeras (PROTACs)[1]. |
T17534 | BCN-PEG4-alkyne | BCN-PEG4-alkyne 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. |
T16249 | N-(Propargyl-PEG4)-N-bis(PEG4-acid) | N-(Propargyl-PEG4)-N-bis(PEG4-acid) is a polyethylene glycol (PEG)-based linker extensively utilized in the synthesis of PROTACs (proteolysis targeting chimeras)[1]. |
T14769 | Br-PEG3-CH2COOH | Br-PEG3-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. |
T17378 | Ald-Ph-amido-C2-nitrate | Ald-Ph-amido-C2-nitrate (Example XXIVb) is a thiazolidine derivative primarily employed as a noncleavable ADC linker[1]. |
T18841 | Thiol-PEG5-alcohol | Thiol-PEG5-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. |
T14814 | Bromo-PEG6-bromide | Bromo-PEG6-bromide 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. |
T16310 | NH2-PEG1-CH2CH2-Boc | NH2-PEG1-CH2CH2-Boc is a polyethylene glycol (PEG) and alkyl/ether-based proteolysis targeting chimeric (PROTAC) linker, commonly employed in the synthesis of PROTACs[1]. |
T17862 | DSPE-PEG46-N3 | DSPE-PEG46-N3 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. |
T17431 | Amino-PEG36-Boc | Amino-PEG36-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. |
T17793 | DBCO-PEG4-Ahx-DM1 | DBCO-PEG4-Ahx-DM1 is a drug-linker conjugate that combines the microtubulin inhibitor DM1 (mertansine), which is an antibody-conjugatable maytansinoid designed to reduce systemic toxicity and improve tumor-specific delivery, with the linker DBCO-PEG4-Ahx, for the development of antibody drug conjugates (ADCs). |
T18524 | PC-PEG11-Azide | PC-PEG11-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. |
T14791 | Bromo-PEG2-C2-Boc | Bromo-PEG2-C2-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. |
T17974 | Fmoc-NH-PEG4-alcohol | Fmoc-NH-PEG4-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. |
T15328 | Fmoc-PEG2-C2-NHS ester | Fmoc-PEG2-CH2CH2-NHS ester is a polyethylene glycol (PEG)-based PROTAC linker designed for the synthesis of proteolysis targeting chimeras (PROTACs). |
T17369 | Ald-Ph-amido-PEG23-OPSS | Ald-Ph-amido-PEG23-OPSS is a cleavable 23-unit polyethylene glycol linker commonly employed for the synthesis of antibody-drug conjugates (ADCs)[1]. |
T17948 | Fmoc-aminooxy-PEG12-NHS ester | Fmoc-aminooxy-PEG12-NHS ester is a polyethylene glycol (PEG) derivative commonly employed as a PROTAC linker for the synthesis of PROTACs[1]. |
T15514 | Hydroxy-PEG10-Boc | Hydroxy-PEG10-Boc is a uncleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Hydroxy-PEG10-Boc can be conjugated to Paclitaxel or docetaxel [2]. |
T16594 | Propargyl-PEG10-amine | Propargyl-PEG10-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. |