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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
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].
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