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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
T14278 Aminooxy-PEG8-acid Aminooxy-PEG8-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.
T16052 Methylamino-PEG4-acid Methylamino-PEG4-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.
T15912 m-PEG6-(CH2)6-Phosphonic acid m-PEG6-(CH2)6-Phosphonic acid serves as a PEG-based PROTAC linker for synthesizing PROTACs[1].
T18416 N-(Hydroxy-PEG3)-N-Boc-PEG4-Boc N-(Hydroxy-PEG3)-N-Boc-PEG4-Boc is a polyethylene glycol (PEG) based linker utilized for the synthesis of PROTACs (proteolysis targeting chimeras)[1].
T14232 Amino-PEG3-C2-acid Amino-PEG3-C2-acid, a cleavable PEG ADC linker, is used in the synthesis of antibody-drug conjugates (ADCs) [1].
T17477 Azido-PEG1-CH2COO-Cl Azido-PEG1-CH2COO-Cl (compound 43a) is an alkyl/ether-based PROTAC linker, commonly employed in the synthesis of PROTAC BRD4 Degrader-1[1].
T17992 H2N-PEG5-Hydrazide H2N-PEG5-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.
T16300 NH-bis(PEG2-propargyl) NH-bis(PEG2-propargyl) 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.
T18714 SPDP-PEG5-acid SPDP-PEG5-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.
T17422 Amino-PEG24-Boc Amino-PEG24-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.
T18422 N-(m-PEG4)-N'-(amino-PEG3)-Cy5 N-(m-PEG4)-N'-(amino-PEG3)-Cy5 is a polyethylene glycol (PEG)-based linker compound employed for synthesizing proteolysis-targeting chimeras (PROTACs)[1].
T15910 m-PEG6-C6-phosphonic acid ethyl ester m-PEG6-C6-phosphonic acid ethyl ester serves as a PEG-based PROTAC linker for the synthesis of PROTACs[1].
T17868 E3 ligase Ligand 10 E3 ligase Ligand 10 serves as a ligand for E3 ubiquitin ligase and can be conjugated to a protein ligand through a linker, resulting in the formation of PROTACs. These PROTACs act as inducers of ubiquitination-mediated degradation, specifically targeting cancer-promoting proteins[1].
T15319 Fmoc-NH-PEG5-CH2COOH Fmoc-NH-PEG5-CH2COOH is a cleavable ADC linker utilized in the synthesis of antibody-drug conjugates (ADCs)[1].
T16187 N-(Azido-PEG3)-N-bis(PEG4-acid) N-(Azido-PEG3)-N-bis(PEG4-acid) is a polyethylene glycol-based linker, designed specifically for the synthesis of PROTACs.[1]
T18763 TCO-PEG3-alcohol TCO-PEG3-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.
T17795 DBCO-PEG4-alkyne DBCO-PEG4-alkyne is a four-unit PEG linker with non-cleavable properties, specifically designed for the synthesis of antibody-drug conjugates (ADCs)[1].
T18483 NH-bis(PEG4-acid) NH-bis(PEG4-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.
T14410 Azido-PEG1-NHS ester Azido-PEG1-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.
T18730 sulfo-SPDB-DM4 Sulfo-SPDB-DM4 is a drug-linker conjugate designed for antibody-drug conjugates (ADCs) that employs the maytansine-based payload (DM4, an antitubulin agent) connected through the sulfo-SPDB linker.
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