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PROTAC Linker

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
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].
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