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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T18205 | m-PEG48-Mal | m-PEG48-Mal 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. |
T14183 | Alkyne-PEG4-maleimide | Alkyne-PEG4-maleimide 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. |
T14000 | [10-(Diethoxy-phosphoryl)-decyl]-phosphonic acid | The compound [10-(diethoxy-phosphoryl)-decyl]-phosphonic acid is a suitable alkyl chain-based PROTAC linker for the synthesis of PROTACs [1]. |
T17678 | Boc-NH-PEG36-CH2CH2COOH | Boc-NH-PEG36-CH2CH2COOH is a polyethylene glycol (PEG)-based PROTAC linker employed for the synthesis of PROTACs[1]. |
T16059 | Methyltetrazine-PEG5-alkyne | Methyltetrazine-PEG5-alkyne, a PEG-based PROTAC linker, is utilized in synthesizing PROTACs[1]. |
T14827 | Bromoacetamido-PEG8-acid | Bromoacetamido-PEG8-acid is a PEG-derived PROTAC linker suitable for synthesizing PROTACs[1]. |
T18278 | Mal-PEG2-VCP-Eribulin | Mal-PEG2-VCP-Eribulin is a chemotherapeutic compound comprising an antibody-drug conjugate (ADC) linker (Mal-PEG2-VCP) and the microtubule inhibitor Eribulin[1]. This compound uniquely targets microtubules, offering a novel approach to cancer treatment. Eribulin is specifically utilized in creating targeted Eribulin-based drugs for antibody conjugates[1]. |
T14725 | Boc-Gly-amido-C-PEG3-C3-amine | Boc-Gly-amido-C-PEG3-C3-amine is a polyethylene glycol (PEG)-based PROTAC linker employed in PROTAC synthesis[1]. |
T16968 | t-Boc-Aminooxy-PEG2-azide | t-Boc-Aminooxy-PEG2-azide is a polyethylene glycol (PEG) derived linker compound employed for the synthesis of proteolysis targeting chimeras (PROTACs)[1]. |
T18015 | HO-PEG4-benzyl ester | HO-PEG4-benzyl 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. |
T17779 | DBCO-PEG1-NHS ester | DBCO-PEG1-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. |
T14629 | Bis-PEG10-acid | Bis-PEG10-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. |
T16455 | PEG3-bis(phosphonic acid diethyl ester) | PEG3-bis(phosphonic acid diethyl ester) is a polyethylene glycol (PEG) derived linker specifically designed for use in the synthesis of proteolysis targeting chimeras (PROTACs)[1]. |
T18511 | OPSS-Val-Cit-PAB-OH | OPSS-Val-Cit-PAB-OH is an ADC linker utilized for the synthesis of antibody-drug conjugates (ADCs) [1]. |
T17578 | Biotin-PEG36-PFP ester | Biotin-PEG36-PFP 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. |
T18625 | Boc-NH-C6-amido-C4-acid | Boc-NH-C6-amido-C4-acid (PROTAC Linker 32) is an alkyl ether-based linker extensively employed in the synthesis of Proteolysis Targeting Chimeras (PROTACs)[1]. |
T15928 | m-PEG8-azide | m-PEG8-azide 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. |
T18780 | TCO-PEG8-amine | TCO-PEG8-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. |
T17479 | Azido-PEG10-Boc | Azido-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. |
T18571 | m-PEG12-2-methylacrylate | Propargyl-PEG13-alcohol is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1]. |