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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T15986 | Mal-PEG3-Boc | Mal-PEG3-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. |
T16189 | N-(Azido-PEG3)-N-Boc-PEG4-acid | N-(Azido-PEG3)-N-Boc-PEG4-acid is a PEG-based PROTAC linker featuring a terminal azide group, primarily employed in PROTAC synthesis[1]. |
T14311 | APN-NH2 | APN- NH2 is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1]. |
T15931 | m-PEG8-(CH2)12-phosphonic acid ethyl ester | m-PEG8-(CH2)12-phosphonic acid ethyl ester is a polyethylene glycol (PEG)-based PROTAC linker, suitable for the synthesis of PROTAC compounds[1]. |
T17586 | Biotin-PEG4-PC-PEG4-alkyne | Biotin-PEG4-PC-PEG4-alkyne is a polyethylene glycol (PEG)-based proteolysis targeting chimera (PROTAC) linker utilized in the synthesis of PROTACs[1]. |
T17463 | Azide-PEG-azide (MW 5000) | Azide-PEG-azide (MW 5000) is a polyethylene glycol (PEG)-based linker component used in the synthesis of proteolysis-targeting chimeras (PROTACs)[1]. |
T14642 | Bis-PEG5-acid | Bis-PEG5-acid (PROTAC Linker 36) is a polyethylene glycol (PEG) linker employed for the synthesis of CP5V, a PROTAC that selectively degrades Cdc20[1]. |
T16645 | Propargyl-PEG7-alcohol | Propargyl-PEG7-alcohol is a PEG-based PROTAC linker utilized in the synthesis of PROTACs [1]. |
T17478 | Azido-PEG1-Val-Cit-OH | Azido-PEG1-Val-Cit-OH is a one-unit cleavable PEG ADC linker employed in the synthesis of antibody-drug conjugates (ADCs)[1]. |
T15862 | m-PEG3-aminooxy-Boc | m-PEG3-ONHBoc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1]. |
T16058 | Methyltetrazine-PEG4-maleimide | Methyltetrazine-PEG4-maleimide is a PEG-based linker that is utilized in PROTAC synthesis[1]. |
T17520 | Azido-PEG8-hydrazide | Azido-PEG8-hydrazide 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. |
T17336 | 4-(N-Boc-amino)-1,6-heptanedioic acid | 4-(N-Boc-amino)-1,6-heptanedioic acid is an alkyl/ether-based linker, suitable for PROTAC synthesis [1]. |
T18268 | Mal-PEG1-Val-Cit-PABC-OH | Mal-PEG1-Val-Cit-PABC-OH is a 1 unit polyethylene glycol (PEG) ADC linker that possesses cleavable properties. This linker, commonly utilized in the synthesis of antibody-drug conjugates (ADCs), serves as a critical component facilitating the conjugation of drugs to antibodies[1]. |
T15763 | Lipoamido-PEG3-OH | Lipoamido-PEG3-OH, also known as compound TA-TEG-G2CN, is a PEG-based PROTAC linker utilized in PROTAC synthesis. It is instrumental in the creation of a robust, dendronized gold nanoparticle (AuNP)-based drug delivery platform[1]. |
T15887 | m-PEG5-2-methylacrylate | m-PEG5-2-methylacrylate is a polyethylene glycol (PEG)- and alkyl/ester-based PROTAC linker employed for the synthesis of proteolysis-targeting chimeras (PROTACs)[1]. |
T16971 | t-Boc-Aminooxy-PEG7-methane | t-Boc-Aminooxy-PEG7-methane is a polyethylene glycol (PEG)-based linker, which finds application in the synthesis of proteolysis targeting chimeras (PROTACs)[1]. |
T17427 | Amino-PEG3-SS-acid | Amino-PEG3-SS-acid is a three-unit polyethylene glycol (PEG) linker that is cleavable. It is commonly employed in the synthesis of antibody-drug conjugates (ADCs)[1]. |
T15762 | Lipoamido-PEG2-OH | Lipoamido-PEG2-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. |
T14422 | Azido-PEG2-hydrazide-Boc | Azido-PEG2-hydrazide-Boc is a polyethylene glycol (PEG) derivative serving as a linker in the development of proteolysis targeting chimeras (PROTACs) [1]. |