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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
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].
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