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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T17087 | THP-SS-alcohol | THP-SS-alcohol is a cleavable linker employed in the synthesis of antibody-drug conjugates (ADCs)[1]. |
T18547 | (+)-Biotin-PEG10-OH | (+)-Biotin-PEG10-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. |
T14112 | Acid-PEG6-mono-methyl ester | Acid-PEG6-mono-methyl ester is a polyethylene glycol (PEG)-based PROTAC linker appropriate for synthesizing PROTACs. [1] |
T17394 | Amine-PEG-amine (MW 5000) | Amine-PEG-amine (MW 5000) is a polyethylene glycol (PEG) based linker utilized in the synthesis of proteolysis-targeting chimeras (PROTACs) [1]. |
T14807 | Bromo-PEG5-bromide | Bromo-PEG5-bromide 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. |
T15974 | Mal-PEG1-Boc | Mal-PEG1-Boc is a alkyl/ether-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. |
T14466 | Azido-PEG6-alcohol | Azido-PEG6-alcohol is a polyethylene glycol (PEG)-based PROTAC linker utilized in PROTAC synthesis[1]. It also functions as a non-cleavable PEG linker consisting of six units, specifically employed in the synthesis of antibody-drug conjugates (ADCs)[2]. |
T17688 | Boc-Phe-(Alloc)Lys-PAB-PNP | Boc-Phe-(Alloc)Lys-PAB-PNP serves as a cleavable linker in the synthesis of antibody-drug conjugates (ADCs). |
T17603 | Bis-Mal-PEG11 | Bis-Mal-PEG11 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. |
T17510 | Azido-PEG36-acid | Azido-PEG36-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. |
T17739 | Cy5-PEG6-NHS ester | Cy5-PEG6-NHS ester (chloride) is a PEG-based PROTAC linker utilized for PROTACs[1] synthesis. |
T18751 | TCO-OH | TCO-OH is a alkyl chain-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. |
T17843 | DOTA-PEG5-amine | DOTA-PEG5-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. |
T14783 | Bromo-PEG1-acid | Bromo-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. |
T14837 | Butane-1,4-diyldiphosphonic acid | Butane-1,4-diyldiphosphonic acid is an alkyl chain-derived linker compound commonly employed in PROTAC synthesis[1]. |
T15979 | Mal-PEG2-alcohol | Mal-PEG2-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. |
T14039 | 4-Bromobutylphosphonic acid | 4-Bromobutylphosphonic acid is an alkyl chain-derived PROTAC linker employed for the synthesis of PROTACs[1]. |
T18183 | m-PEG3-S-PEG4-propargyl | m-PEG3-S-PEG4-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. |
T15125 | Diethylene Glycol Monobenzyl Ether | Diethylene Glycol Monobenzyl Ether is a PEG-based linker, specifically designed for the synthesis of PROTACs[1]. It serves as a versatile chemical compound, enabling the formation of PROTAC molecules by connecting target protein ligands with E3 ligase ligands, ultimately leading to targeted protein degradation. |
T14105 | Acid-PEG4-C2-Boc | Acid-PEG4-C2-Boc is a linker compound based on polyethylene glycol (PEG) and alkyl/ether. It is utilized in the synthesis of PROteolysis TArgeting Chimeras (PROTACs) for the purpose of inhibiting the mechanistic Target of Rapamycin (mTOR)[1]. |