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
T15475	Hexaethylene glycol monomethyl ether	Hexaethylene glycol monomethyl ether, a PEG-based PROTAC linker, facilitates the synthesis of PROTACs[1].
T18550	(+)-Biotin-PEG6-hydrazide	(+)-Biotin-PEG6-hydrazide is a polyethylene glycol (PEG) derived linker, specifically designed for the synthesis of proteolysis-targeting chimeras (PROTACs)[1].
T17529	BCN-PEG3-Biotin	BCN-PEG3-Biotin is a non-cleavable three-unit PEG linker employed in the synthesis of antibody-drug conjugates (ADCs)[1].
T18040	Hydroxy-PEG20-Boc	Hydroxy-PEG20-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.
T14730	Boc-N-Amido-PEG4-propargyl	Boc-N-Amido-PEG4-propargyl is a PEG-based PROTAC linker utilized for synthesizing PROTACs[1].
T17761	DBCO-NHCO-PEG13-acid	DBCO-NHCO-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.
T14636	Bis-PEG3-PFP ester	Bis-PEG3-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.
T17646	Boc-C1-PEG3-C4-OBn	Boc-C1-PEG3-C4-OBn (PROTAC Linker 15) is a PEG-based PROTAC linker employed in the synthesis of various PROTACs, including PROTAC SGK3 degrader-1. PROTACs are composed of two distinct ligands connected by a linker; one ligand binds to an E3 ubiquitin ligase, while the other specifically interacts with the target protein. By leveraging the intracellular ubiquitin-proteasome system, PROTACs can selectively degrade target proteins[1].
T16611	Propargyl-PEG3-phosphonic acid diethyl ester	Propargyl-PEG3-phosphonic acid diethyl ester, a PEG-based PROTAC linker, is employed for the synthesis of PROTACs[1].
T14582	Biotin-PEG2-acid	Biotin-PEG2-acid, a non-cleavable 2-unit PEG ADC linker, is utilized in the synthesis of antibody-drug conjugates (ADCs)[1].
T18357	Methyltetrazine-PEG8-PFP ester	Methyltetrazine-PEG8-PFP ester is a PEG-based PROTAC linker utilized for the synthesis of PROTACs[1].
T15059	DBCO-C6-acid	DBCO-C6-acid is a non-cleavable linker utilized for the synthesis of antibody-drug conjugates (ADCs) and carmaphycin analogues[1].
T18462	N-(Propanoic acid)-N-bis(m-PEG12)	N-(Propanoic acid)-N-bis(m-PEG12) is a polyethylene glycol (PEG) based linker for PROTACs synthesis[1].
T16619	Propargyl-PEG4-Br	Propargyl-PEG4-Br is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
T18310	AZ1508	AZ1508, a tubulin inhibitor[1], serves as a drug-linker conjugate for antibody-drug conjugates (ADC) targeting breast and stomach cancer treatment.
T17814	DBCO-Val-Cit-OH	DBCO-Val-Cit-OH, a cleavable linker compound, finds utility in the synthesis of antibody-drug conjugates (ADCs)[1].
T18138	m-PEG12-DSPE	m-PEG12-DSPE 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.
T17119	Tos-aminoxy-Boc-PEG4-Tos	Tos-aminoxy-Boc-PEG4-Tos is a PEG4-based PROTAC linker utilized for the synthesis of PROTACs[1].
T16653	Propargyl-PEG9-amine	Propargyl-PEG9-amine, a PEG-based PROTAC linker, can be utilized in the synthesis of PROTACs.
T17824	Diketone-PEG11-Diketone	Diketone-PEG11-Diketone is a polyethylene glycol (PEG)-based linker utilized for the synthesis of proteolysis-targeting chimeras (PROTACs)[1].

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PROTAC Linker