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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
T14170 Ald-Ph-PEG6-Boc Ald-Ph-PEG6-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.
T14257 Aminoethyl-SS-ethylalcohol Aminoethyl-SS-ethylalcohol (Compound 3) is an Alkyl-Chain-based PROTAC linker can be used in the synthesis of PROTACs[1]. Aminoethyl-SS-ethylalcohol is also a glutathione cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[2].
T14718 Boc-Aminooxy-PEG4-CH2CO2H Boc-Aminooxy-PEG4-CH2CO2H is a polyethylene glycol (PEG) derivative serving as a PROTAC linker for the synthesis of proteolysis targeting chimeras (PROTACs)[1].
T15331 Fmoc-PEG4-Ala-Ala-Asn-PAB Fmoc-PEG4-Ala-Ala-Asn-PAB is a four-unit polyethylene glycol (PEG) linker, cleavable in nature. It is specifically employed for the synthesis of antibody-drug conjugates (ADCs)[1].
T17658 Boc-NH-PEG-amine (MW 5000) Boc-NH-PEG-amine (MW 5000) is a PEG-based PROTAC linker enabling the synthesis of PROTACs [1].
T17343 7-O-(Amino-PEG4)-paclitaxel 7-O-(Amino-PEG4)-paclitaxel 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.
T17366 Ald-CH2-PEG10-Boc Ald-CH2-PEG10-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.
T18869 Vat-Cit-PAB-Monomethyl Dolastatin 10 Vat-Cit-PAB-Monomethyl Dolastatin 10 is an ADC linker-conjugated drug designed to deliver potent antitumor activity. It achieves this through Monomethyl Dolastatin 10, a potent tubulin inhibitor, connected via the Vat-Cit-PAB ADC linker.
T15997 Mal-PEG5-NHS ester Mal-PEG5-NHS ester, an alkyl/ether and PEG-based PROTAC linker, is utilized for the synthesis of PROTACs.
T14248 Amino-PEG7-amine Amino-PEG7-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.
T18116 m-PEG-triethoxysilane (MW 5000) m-PEG-triethoxysilane (MW 5000) is a polyethylene glycol-based PROTAC linker suitable for the synthesis of PROTACs[1].
T18291 Mal-PEG4-Val-Cit-PAB Mal-PEG4-Val-Cit-PAB, a cleavable ADC linker incorporating a Maleimide moiety, finds application in the construction of antibody-drug conjugates (ADCs)[1].
T18177 m-PEG3-amido-C3-triethoxysilane m-PEG3-amido-C3-triethoxysilane is a polyethylene glycol (PEG)-based linker commonly utilized in the synthesis of proteolysis-targeting chimeras (PROTACs)[1].
T15959 Mal-amido-PEG6-NHS ester Mal-amido-PEG6-NHS ester is a polyethylene glycol (PEG)-based linker, specifically designed for the synthesis of proteolysis-targeting chimeras (PROTACs)[1].
T18106 m-PEG-OH (MW5000) m-PEG-OH (MW5000) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
T17445 Aminooxy-amido-PEG4-propargyl Aminooxy-amido-PEG4-propargyl is a 4-unit PEG ADC linker that is non-cleavable and specifically designed for the synthesis of antibody-drug conjugates (ADCs)[1].
T18497 NHPI-PEG2-C2-Pfp ester NHPI-PEG2-C2-Pfp ester is a noncleavable 2-unit polyethylene glycol (PEG) linker widely employed in the synthesis of antibody-drug conjugates (ADCs).
T17866 DSPE-PEG5-propargyl DSPE-PEG5-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.
T16588 Propargyl-PEG1-SS-alcohol Propargyl-PEG1-SS-alcohol is a 1-unit PEG ADC linker that is cleavable. It finds application in the synthesis of antibody-drug conjugates (ADCs)[1].
T17938 endo-BCN-PEG4-Val-Cit-PAB-MMAE Endo-BCN-PEG4-Val-Cit-PAB-MMAE is a cleavable four-unit polyethylene glycol (PEG) linker, specifically designed for the synthesis of antibody-drug conjugates (ADCs)[1].
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