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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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. |