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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T14633 | Bis-PEG2-PFP ester | Bis-PEG2-PFP ester is a non-cleavable 2-unit polyethylene glycol (PEG) linker employed in the synthesis of antibody-drug conjugates (ADCs) [1]. Additionally, Bis-PEG2-PFP ester serves as a PEG-based linker for the synthesis of proteolysis targeting chimeras (PROTACs) [2]. |
T17804 | DBCO-PEG5-DBCO | DBCO-PEG5-DBCO 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. |
T15148 | DNP-NH-PEG2-C2-acid | DNP-NH-PEG2-C2-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. |
T17370 | Ald-Ph-amido-PEG24-acid | Ald-Ph-amido-PEG24-acid is a polyethylene glycol (PEG)-based linker used for the synthesis of proteolysis targeting chimeras (PROTACs)[1]. |
T16167 | N-(4-Carboxycyclohexylmethyl)maleimide | N-(4-Carboxycyclohexylmethyl)maleimide is an alkyl chain-based PROTAC linker suitable for synthesizing PROTACs[1]. |
T17599 | Bis-Bromoacetamido-PEG11 | Bis-Bromoacetamido-PEG11 is a polyethylene glycol (PEG) derived linker compound, specifically designed for the synthesis of PROTACs[1]. |
T14535 | Benzyl-PEG2-CH2-Boc | Benzyl-PEG2-CH2-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. |
T17961 | Fmoc-N-PEG24-acid | Fmoc-N-PEG24-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. |
T18210 | m-PEG5-triethoxysilane | m-PEG5-triethoxysilane 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. |
T15859 | m-PEG3-NHS ester | m-PEG3-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. |
T18832 | Thiol-PEG-CH2COOH (MW 2000) | Thiol-PEG-CH2COOH (MW 2000) is a PEG-based PROTAC linker utilized for synthesizing PROTACs[1]. |
T17558 | Biotin-PEG11-oxyamine | Biotin-PEG11-oxyamine 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. |
T18821 | Thalidomide-O-amido-PEG4-azide | Thalidomide-O-amido-PEG4-azide is a polyethylene glycol (PEG) derivative serving as a linker for Proteolysis Targeting Chimeras (PROTACs) synthesis [1]. |
T18581 | Propargyl-peg3-sulfone-peg3-propargyl | Propargyl-PEG3-sulfone-PEG3-propargyl is a polyethylene glycol (PEG)-based linker specifically designed for the synthesis of proteolysis-targeting chimeras (PROTACs)[1]. |
T15965 | Mal-amido-PEG9-amine | Mal-amido-PEG9-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. |
T16228 | N-Mal-N-bis(PEG2-amine) | N-Mal-N-bis(PEG2-amine) is a polyethylene glycol (PEG)-based linker compound commonly employed in the construction of PROTACs, or proteolysis-targeting chimeras[1]. |
T18700 | SPB | SPB is a potent anti-inflammatory drug-linker conjugate for Antibody-Drug Conjugates (ADC), utilizing Xanthotoxol connected through the ADC linker. |
T16229 | N-Mal-N-bis(PEG2-C2-Boc) | N-Mal-N-bis(PEG2-C2-Boc) is a polyethylene glycol (PEG)-based linker for proteolysis targeting chimeras (PROTACs)[1]. |
T17632 | Bis-propargyl-O-PEG17 | Bis-propargyl-O-PEG17 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. |
T18326 | MC-Val-Cit-PAB-MMAF | MC-Val-Cit-PAB-MMAF is an antibody-drug conjugate (ADC) component that exhibits antitumor properties through the action of the tubulin inhibitor, monomethyl auristatin F (MMAF), which is connected by a cathepsin-cleavable linker, MC-Val-Cit-PAB. |