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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T18736 | SuO-Val-Cit-PAB-MMAE | SuO-Val-Cit-PAB-MMAE is an ADC (antibody-drug conjugate) linker comprising the anti-mitotic monomethyl auristatin E (MMAE, a tubulin inhibitor) connected through the SuO-Val-Cit-PAB peptide. |
T14805 | Bromo-PEG5-azide | Bromo-PEG5-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. |
T15295 | Fluorescein-PEG6-bis-NHS ester | Fluorescein-PEG6-bis-NHS ester is a polyethylene glycol (PEG)-based linker used for the synthesis of proteolysis targeting chimeras (PROTACs)[1]. |
T14821 | Bromoacetamido-PEG3-C2-Boc | Bromoacetamido-PEG3-C2-Boc is a polyethylene glycol (PEG) derived linker that is suitable for the synthesis of proteolysis-targeting chimeras (PROTACs) [1]. |
T18182 | m-PEG3-S-PEG3-Boc | m-PEG3-S-PEG3-Boc is a polyethylene glycol (PEG) and alkyl/ether-based linker utilized in the synthesis of PROteolysis TArgeting Chimeras (PROTACs)[1]. |
T16827 | S-acetyl-PEG6-Tos | S-acetyl-PEG6-Tos 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. |
T17052 | Tetraethyl heptane-1,7-diylbis(phosphonate) | Tetraethyl heptane-1,7-diylbis(phosphonate) is an alkyl chain-derived PROTAC linker, commonly employed for PROTAC synthesis[1]. |
T14098 | Acid-PEG1-C2-Boc | Acid-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. |
T14310 | APN-C3-PEG4-azide | APN-C3-PEG4-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. |
T17349 | Ac4GlcNAlk | Ac4GlcNAlk is a alkyl chain-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. |
T15510 | Hydroxy-PEG1-acid | Hydroxy-PEG1-acid is a non-cleavable 1-unit polyethylene glycol (PEG) linker utilized for the synthesis of antibody-drug conjugates (ADCs)[1]. |
T18243 | Mal-amido-PEG5-C2-NHS ester | Mal-amido-PEG10-C2-NHS ester is a noncleavable ADC linker, comprising a maleimide group and an NHS ester, which serves as a labeling agent for primary amines (-NH2) found in proteins, amine-modified oligonucleotides, and other amine-containing molecules[1][2]. |
T17003 | TBDMS-PEG4-OH | TBDMS-PEG4-OH 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. |
T14889 | Cbz-NH-PEG4-C2-acid | Cbz-NH-PEG4-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. |
T16652 | Propargyl-PEG8-OH | Propargyl-PEG8-OH 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. |
T18495 | NH2-PEG8-C1-Boc | NH2-PEG8-C1-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. |
T15992 | Mal-PEG4-OH | Mal-PEG4-OH 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. |
T14597 | Biotin-PEG4-acid | Biotin-PEG4-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. |
T15940 | m-PEG9-Amine | m-PEG9-Amine is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1]. |
T17965 | Fmoc-NH-PEG11-CH2CH2COOH | Fmoc-NH-PEG11-CH2CH2COOH, a PEG-based PROTAC linker, serves as a valuable tool in PROTAC synthesis[1]. |