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
T16024	MC-GGFG-DX8951	MC-GGFG-DX8951 is a drug-linker conjugate designed for antibody-drug conjugation (ADC) that demonstrates antitumor activity through the deployment of DX8951, a DNA topoisomerase I inhibitor, connected using the protease-cleavable MC-GGFG linker[1].
T18789	Tetrazine-PEG4-biotin	Tetrazine-PEG4-biotin is a cleavable linker composed of a four-unit PEG (polyethylene glycol) chain. This compound is specifically designed for use in the synthesis of antibody-drug conjugates (ADCs)[1].
T15320	Fmoc-NH-PEG6-CH2CH2COOH	Fmoc-NH-PEG6-CH2CH2COOH is a cleavable linker commonly employed in the synthesis of antibody-drug conjugates (ADCs)[1].
T14457	Azido-PEG5-amine	Azido-PEG5-amine 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.
T16149	Ms-PEG4-Ms	Ms-PEG4-Ms 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.
T18764	TCO-PEG3-amide-C3-triethoxysilane	TCO-PEG3-amide-C3-triethoxysilane is a polyethylene glycol (PEG)-based linker for proteolysis targeting chimeras (PROTACs) synthesis[1].
T18253	Mal-NH-PEG10-CH2CH2COOPFP ester	Mal-NH-PEG10-CH2CH2COOPFP ester is a polyethylene glycol (PEG)-based linker molecule employed in the synthesis of proteolysis targeting chimeras (PROTACs)[1].
T18175	m-PEG25-NHS ester	m-PEG25-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.
T17446	Aminooxy-PEG-OH (MW 2000)	Aminooxy-PEG-OH (MW 2000) serves as a PEG-based PROTAC linker for the synthesis of PROTACs[1].
T15528	Hydroxy-PEG4-acid	Hydroxy-PEG4-acid, a non-cleavable 4-unit PEG ADC linker, is utilized in the synthesis of antibody-drug conjugates (ADCs) [1].
T18256	Mal-NH-PEG16-CH2CH2COOPFP ester	Mal-NH-PEG16-CH2CH2COOPFP ester is a polyethylene glycol-based linker, designed for the synthesis of proteolysis targeting chimeras (PROTACs) [1].
T17770	DBCO-NHCO-PEG6-amine	DBCO-NHCO-PEG6-amine 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.
T15227	endo-BCN-PEG4-Boc	endo-BCN-PEG4-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.
T16001	Mal-PEG6-NHS ester	Mal-PEG6-NHS ester is a noncleavable ADC linker consisting of a Maleimide functional group, a 6-unit Polyethylene Glycol (PEG) spacer, and an N-Hydroxysuccinimide (NHS) ester moiety.
T17140	Tos-PEG9-Boc	Tos-PEG9-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.
T17432	Amino-PEG36-CH2-Boc	Amino-PEG36-CH2-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.
T15961	Mal-amido-PEG8-C2-acid	Mal-amido-PEG8-C2-acid (US2018339985, example 142) is a noncleavable linker for antibody-drug conjugates (ADCs) [1].
T17396	Amine-PEG-CH2COOH (MW 3400)	Amine-PEG-CH2COOH (MW 3400) is a polyethylene glycol (PEG)-based linker used in the synthesis of proteolysis targeting chimeras (PROTACs)[1].
T14644	Bis-PEG5-PFP ester	Bis-PEG5-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.
T17806	DBCO-PEG8-acid	DBCO-PEG8-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