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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
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.
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