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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
T16047 Methylamino-PEG1-acid Methylamino-PEG1-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.
T17460 Azide-PEG-azide (MW 10000) Azide-PEG-azide (MW 10000) is a polyethylene glycol (PEG)-based linker for PROTACs synthesis. It serves as an essential component in assembling PROTAC molecules[1].
T14029 3,6-Dioxaoctanedioic acid 3,6-dioxaoctanedioic acid serves as a PEG-based PROTAC linker for the synthesis of PROTACs[1].
T14394 Azide-PEG3-Tos Azide-PEG3-Tos is a PEG-based PROTAC linker utilized in the synthesis of PROTACs[1]. It is a non-cleavable 3 unit PEG ADC linker employed in the synthesis of antibody-drug conjugates (ADCs)[2].
T16646 Propargyl-PEG7-Boc Propargyl-PEG7-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.
T14819 Bromoacetamido-PEG3-azide Bromoacetamido-PEG3-azide is a polyethylene glycol (PEG)-based linker used for the synthesis of proteolysis-targeting chimeras (PROTACs)[1].
T17504 Azido-PEG3-S-PEG4-t-butyl ester Azido-PEG3-S-PEG4-t-butyl ester is a PEG-based PROTAC linker employed for PROTAC synthesis[1].
T17802 DBCO-PEG4-VC-PAB-DMEA-PNU-159682 DBCO-PEG4-VC-PAB-DMEA-PNU-159682, a drug-linker conjugate for antibody-drug conjugates (ADC), comprises the ADC linker DBCO-PEG4-VC-PAB and the potent ADC cytotoxin DMEA-PNU-159682. The cytotoxin includes metabolites of nemorubicin (MMDX) from liver microsomes and the ADC cytotoxin PNU-159682[1].
T17570 Biotin-PEG24-acid Biotin-PEG24-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.
T15836 m-PEG10-azide m-PEG10-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.
T17758 DBCO-NHCO-PEG12-amine DBCO-NHCO-PEG12-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.
T15318 Fmoc-NH-PEG4-CH2COOH Fmoc-NH-PEG4-CH2COOH is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs) [1].
T18536 PEG7-O-Ms PEG7-O-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.
T18109 m-PEG-thiol (MW 2000) m-PEG-thiol (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.
T14268 Aminooxy-PEG3-methyl ester Aminooxy-PEG3-methyl ester, a PEG-based PROTAC linker, serves as a pivotal element in the synthesis of PROTACs[1].
T14400 Azide-PEG8-alcohol Azide-PEG8-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.
T18327 MC-Val-Cit-PAB-Retapamulin MC-Val-Cit-PAB-Retapamulin is a drug-linker conjugate for antibody-drug conjugates (ADC) that exhibits potent antitumor activity. This compound utilizes Retapamulin, a ribosome inhibitor, connected through the ADC linker MC-Val-Cit-PAB.
T18193 m-PEG36-Br m-PEG36-Br 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.
T14701 BnO-PEG5-OH BnO-PEG5-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.
T15765 Lipoamido-PEG4-azide Lipoamido-PEG4-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.
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