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]. |