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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T18741 | t-Boc-Aminooxy-PEG4-NHS ester | t-Boc-Aminooxy-PEG4-NHS ester is a polyethylene glycol (PEG) derivative, functioning as a linker for PROTAC synthesis[1]. |
T17616 | Bis-PEG13-acid | Bis-PEG13-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. |
T17778 | DBCO-PEG1-NH-Boc | DBCO-PEG1-NH-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. |
T17485 | Azido-PEG12-Boc | Azido-PEG12-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. |
T14595 | Biotin-PEG3-oxyamine | Biotin-PEG3-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. |
T18506 | NO2-SPP-sulfo-Me | NO2-SPP-sulfo-Me is a cleavable linker utilized in the synthesis of antibody-drug conjugates (ADC)[1]. |
T18742 | t-Boc-Aminooxy-PEG5-azide | t-Boc-Aminooxy-PEG5-azide is a polyethylene glycol (PEG) derivative that serves as a linker for the synthesis of proteolysis-targeting chimeras (PROTACs)[1]. |
T17711 | Cbz-aminooxy-PEG8-acid | Cbz-aminooxy-PEG8-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. |
T18792 | Tetrazine-PEG4-SS-Py | Tetrazine-PEG4-SS-Py is a cleavable PEG ADC linker comprising four units. It is specifically designed for the synthesis of antibody-drug conjugates (ADCs)[1]. |
T14467 | Azido-PEG6-amine | Azido-PEG6-amine is a polyethylene glycol (PEG)-based linker compound commonly employed in the synthesis of Proteolysis Targeting Chimeras (PROTACs)[1]. Additionally, it serves as a non-cleavable 6-unit PEG linker in the synthesis of antibody-drug conjugates (ADCs)[2]. |
T18331 | MC-VC-PABC-DNA31 | MC-VC-PABC-DNA31 is a drug-linker conjugate designed for Antibody-Drug Conjugates (ADC) that demonstrates potent antitumor activity. It employs DNA31, an effective inhibitor of RNA polymerase, connected through the MC-VC-PABC ADC linker. |
T15225 | endo-BCN-PEG3-NH-Boc | endo-BCN-PEG3-NH-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. |
T17800 | DBCO-PEG4-triethoxysilane | DBCO-PEG4-triethoxysilane is a polyethylene glycol (PEG)-based linker compound that serves as an efficient building block for the synthesis of PROTACs. These PROTACs are small molecules designed to selectively target and degrade specific proteins of interest[1]. |
T16613 | Propargyl-PEG4-5-nitrophenyl carbonate | Propargyl-PEG4-5-nitrophenyl carbonate is a polyethylene glycol (PEG) derivative specifically designed as a linker for proteolysis targeting chimeras (PROTACs) synthesis[1]. |
T18829 | Thalidomide-O-PEG4-Boc | Thalidomide-O-PEG4-Boc is a PEG-based PROTAC linker utilized in PROTAC synthesis [1]. |
T201925 | 7-Bromohept-1-yne | 7-Bromohept-1-yne是一种PROTAC Linker,可用于合成AK-1690,一种STAT6(Signal transducer and activator of transcription 6) PROTAC降解物。 |
T14483 | Azido-PEG9-Boc | Azido-PEG9-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. |
T203812 | Alkyne-PEG6-acid | Alkyne-PEG6-acid 是一种具有异功能性的 PEG 化交联剂,应用于生物偶联和小分子合成中,作为组分使用。该交联剂一端含有羧基,另一端则为炔烃基团。在 PROTACs 中使用时称为 2-2-2-2-2-2-6 PROTAC链接剂,也用于抗体药物偶联物的合成。 |
T18180 | m-PEG3-S-PEG1-C2-Boc | m-PEG3-S-PEG1-C2-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. |
T14393 | Azide-PEG3-C1-Ala | Azide-PEG3-C1-Ala 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. |