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
T15834	m-PEG10-alcohol	m-PEG10-alcohol, also known as Decaethylene glycol monomethyl ether, is a non-cleavable 10 unit PEG ADC linker utilized in the synthesis of antibody-drug conjugates (ADCs)[1]. Additionally, m-PEG10-alcohol serves as a PEG-based PROTAC linker, enabling its application in the synthesis of PROTACs[1].
T14428	Azido-PEG3-CH2CO2Me	Azido-PEG3-CH2CO2Me 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.
T17954	Fmoc-Lys (biotin-PEG12)-OH	Fmoc-Lys (biotin-PEG12)-OH is a PEGylation-based linker compound utilized in PROTAC synthesis[1].
T17626	Bis-PEG25-acid	Bis-PEG25-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.
T17531	BCN-PEG3-Val-Cit	BCN-PEG3-Val-Cit is a PEG-based linker commonly employed in PROTAC synthesis[1]. Additionally, it serves as a cleavable 3 unit PEG linker in the production of antibody-drug conjugates (ADCs)[2].
T17826	Diketone-PEG12-Biotin	Diketone-PEG12-Biotin 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.
T17126	Tos-PEG4-acid	Tos-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.
T17972	Fmoc-NH-PEG3-C2-NH2	Fmoc-NH-PEG3-C2-NH2 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.
T16317	NH2-PEG7	NH2-PEG7 is a para-aminomethylbenzyloxycarbonyl (PROTAC) linker compound consisting of a polyethylene glycol (PEG) chain. It finds application in the synthesis of the PROTAC PARP1 degrader called iRucaparib-AP6[1].
T14159	Ald-CH2-PEG5-azide	Ald-CH2-PEG5-azide is a non-cleavable linker consisting of a five unit PEG chain, commonly employed in the synthesis of antibody-drug conjugates (ADCs)[1].
T16438	PC Biotin-PEG3-azide	PC Biotin-PEG3-azide is a cleavable three-unit polyethylene glycol (PEG) antibody-drug conjugate (ADC) linker, employed in the synthesis of ADCs[1].
T17956	Fmoc-N-bis-PEG3-NH-Boc	Fmoc-N-bis-PEG3-NH-Boc is a cleavable ADC linker compound consisting of three PEG units, employed in the synthesis of antibody-drug conjugates (ADCs)[1].
T17523	Azido-PEG9-NHS ester	Azido-PEG9-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.
T16659	Boc-NH-PEG2-C2-NH2	Boc-NH-PEG2-C2-NH2 (PROTAC Linker 13) is a PEG-based linker utilized for the synthesis of PROTACs. This chemical compound plays a crucial role in connecting the targeted protein and the E3 ubiquitin ligase for selective protein degradation[1].
T15299	Fluorescein-thiourea-PEG6-acid	Fluorescein-thiourea-PEG6-acid is a polyethylene glycol (PEG) derived linker commonly employed in the synthesis of proteolysis targeting chimeras (PROTACs) [1].
T18089	m-PEG-CH2COOH (MW 5000)	m-PEG-CH2COOH (MW 5000) is a polyethylene glycol (PEG) derived PROTAC linker, employed in the synthesis of PROTACs. [1]
T18828	Thalidomide-O-PEG4-azide	Thalidomide-O-PEG4-azide is a PEG-based PROTAC linker utilized in PROTAC synthesis[1].
T18323	MC-Val-Cit-PAB-dimethylDNA31	MC-Val-Cit-PAB-dimethylDNA31 is a drug-linker conjugate employed in antibody-drug conjugates (ADCs) that exhibits robust antitumor efficacy. This conjugate utilizes the ADC linker, MC-Val-Cit-PAB, to link to the potent antitumor agent dimethylDNA31. Notably, dimethylDNA31 also demonstrates significant bactericidal activity against both persister and stationary-phase Staphylococcus aureus.
T18840	Thiol-PEG5-acid	Thiol-PEG5-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.
T18674	(S,R,S)-AHPC-PEG2-acid	(S,R,S)-AHPC-PEG2-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