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 | |
---|---|---|
T16062 | Methyltetrazine-PEG8-NHS ester | Methyltetrazine-PEG8-NHS ester is a polyethylene glycol (PEG) derivative, specifically designed as a PROTAC linker for the synthesis of Proteolysis Targeting Chimeras (PROTACs)[1]. |
T14097 | Acid-C2-PEG4-C2-NHS ester | Acid-C2-PEG4-C2-NHS ester, a PEG-based PROTAC linker, facilitates the synthesis of PROTACs[1]. |
T17154 | Tr-PEG8-OH | Tr-PEG8-OH, a non-cleavable 8-unit PEG ADC linker, is utilized in the synthesis of antibody-drug conjugates (ADCs). |
T18297 | Mal-PEG6-mal | Mal-PEG6-mal 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. |
T18731 | Sulfo-PDBA-DM4 | Sulfo-PDBA-DM4 is a drug-linker conjugate for antibody-drug conjugate (ADC) applications, combining the potent tubulin inhibitor DM4 with the gluthatione-cleavable linker Sulfo-PDBA. This configuration harnesses DM4's cytotoxic potential through Sulfo-PDBA's targeted delivery mechanism. |
T18275 | Mal-PEG16-NHS ester | Mal-PEG16-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. |
T17374 | Ald-Ph-PEG2-Boc | Ald-Ph-PEG2-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. |
T14020 | (2-Pyridyldithio)-PEG4-propargyl | (2-Pyridyldithio)-PEG4-propargyl is a polyethylene glycol (PEG)-based linker specifically designed for use in the synthesis of proteolysis-targeting chimeras (PROTACs) [1]. |
T16318 | NH2-PEG8-OH | NH2-PEG8-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. |
T18336 | Methylcyclopropene-PEG4-NHS | Methylcyclopropene-PEG4-NHS is a four-unit PEG ADC linker, which can be cleaved. It is utilized in the synthesis of antibody-drug conjugates (ADCs)[1]. |
T16227 | N-Mal-N-bis(PEG2-acid) | N-Mal-N-bis(PEG2-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. |
T18797 | Tetrazine-Ph-NHCO-PEG4-NH-Boc | Tetrazine-Ph-NHCO-PEG4-NH-Boc is a PEGylated PROTAC linker suitable for PROTAC synthesis[1]. |
T17799 | DBCO-PEG4-SS-TCO | DBCO-PEG4-SS-TCO is a cleavable 4-unit polyethylene glycol (PEG) linker essential for the synthesis of antibody-drug conjugates (ADCs)[1]. It plays a crucial role in connecting the drug payload to the antibody, enabling targeted drug delivery. |
T14648 | Bis-PEG7-NHS ester | Bis-PEG7-NHS ester is a cleavable ADC linker utilized in the synthesis of antibody-drug conjugates (ADCs) [1]. |
T18067 | Lenalidomide-PEG1-azide | Lenalidomide-PEG1-azide is an E3 ligase ligand-linker conjugate that incorporates the cereblon ligand based on Lenalidomide and a linker. It is designed for use in the development of PROTAC BRD4 Degrader-2[1]. |
T18241 | Mal-amido-PEG24-acid | Mal-amido-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. |
T18583 | Propargyl-PEG4-S-PEG4-acid | Propargyl-PEG4-S-PEG4-acid is a polyethylene glycol (PEG)-based PROTAC linker, suitable for the synthesis of Proteolysis Targeting Chimera (PROTACs)[1]. |
T17425 | Amino-PEG27-amine | Amino-PEG27-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. |
T14013 | 2-(Benzyloxy)ethanol | 2-(Benzyloxy)ethanol 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. |
T18320 | MC-Val-Cit-PAB-carfilzomib iodide | MC-Val-Cit-PAB-carfilzomib is a potent antitumor drug-linker conjugate for antibody-drug conjugates (ADC), comprising the irreversible proteasome inhibitor carfilzomib, connected through the ADC linker MC-Val-Cit-PAB. |