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
T17929	EC089	EC089 is a cleavable linker employed in tubulysins and folates conjugates[1].
T16661	NH2-PEG5-C2-NH-Boc	NH2-PEG5-C2-NH-Boc (PROTAC Linker 17) is a PEG-based compound utilized as a linker in the synthesis of PROTACs[1].
T14731	Boc-N-PEG1-C2-NHS ester	Boc-N-PEG1-C2-NHS ester, a PEG-based linker, finds utility in PROTAC synthesis[1].
T17449	APN-PEG4-Amine hydrochloride	APN-PEG4-Amine (hydrochloride) is a cleavable four-unit polyethylene glycol (PEG) linker utilized in the synthesis of antibody-drug conjugates (ADCs)[1].
T16627	Propargyl-PEG4-methylamine	Propargyl-PEG4-methylamine is a polyethylene glycol (PEG) derived linker essential for the synthesis of Proteolysis Targeting Chimeras (PROTACs)[1].
T17536	BCN-PEG4-NHS ester	BCN-PEG4-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.
T14659	Bis-propargyl-PEG6	Bis-propargyl-PEG6 is a polyethylene glycol (PEG) derivative commonly employed as a PEG-based PROTAC linker during the synthesis of PROTACs. Its application includes the generation of polymer-linked multimers of guanosine-3', 5'-cyclic monophosphates[1].
T18782	TCO-PEG8-TCO	TCO-PEG8-TCO 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.
T16233	N-Mal-N-bis(PEG4-NH-Boc)	N-Mal-N-bis(PEG4-NH-Boc) is a PEG-based PROTAC linker utilized for synthesizing PROTACs[1].
T14032	3-Maleimidopropionic acid	3-Maleimidopropionic acid is an alkyl chain-derived PROTAC linker employed in PROTAC synthesis[1].
T18121	m-PEG10-NHS ester	m-PEG10-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.
T18586	Propargyl-PEG4-Sulfone-PEG4-acid	Propargyl-PEG4-Sulfone-PEG4-acid serves as a PEG-based PROTAC linker for the synthesis of PROTACs[1].
T17400	Amine-PEG-thiol (MW 5000)	Amine-PEG-thiol (MW 5000) is a polyethylene glycol (PEG) based PROTAC linker, primarily utilized for the synthesis of PROTACs[1].
T15918	m-PEG6-Tos	m-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.
T14787	Bromo-PEG2-alcohol	Bromo-PEG2-alcohol 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.
T16195	N-(Azido-PEG4)-N-bis(PEG4-acid)	N-(Azido-PEG4)-N-bis(PEG4-acid) is a polyethylene glycol (PEG) derived PROTAC linker, facilitating PROTAC synthesis[1].
T18358	Methyltetrazine-SS-NHS	Methyltetrazine-SS-NHS is a cleavable ADC linker employed for the synthesis of antibody-drug conjugates (ADCs)[1].
T18141	m-PEG12-NH-C2-acid	m-PEG12-NH-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.
T14784	Bromo-PEG1-C2-Boc	Bromo-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.
T17615	Bis-PEG12-acid	Bis-PEG12-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.

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PROTAC Linker