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
T18720	FCHFHS-ST7612AA1	FCHFHS-ST7612AA1 is a part of antibody drug conjugates (ADCs) charged with HDAC inhibitor by a linker, shows antitumor activity[1].
T16172	N-(Amino-PEG4)-N-bis(PEG4-Boc)	N-(Amino-PEG4)-N-bis(PEG4-Boc) is a polyethylene glycol (PEG)-based linker, utilized for the synthesis of proteolysis targeting chimeras (PROTACs)[1].
T17454	ATP-polyamine-biotin	ATP-polyamine-biotin is a cell-permeable, efficient kinase cosubstrate with conversions and kinetics similar to those of other known ATP analogues. APB shows a cytotoxicity EC50 value of 19 ± 1 mM. ATP-polyamine-biotin is shown to promote biotin labeling
T14412	Azido-PEG10-acid	Azido-PEG10-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.
T15291	Fluorescein-PEG3-amine	Fluorescein-PEG3-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.
T18220	m-PEG8-ethoxycarbonyl-NHS ester	m-PEG8-ethoxycarbonyl-NHS ester is a polyethylene glycol (PEG)-based linker, utilized for the synthesis of PROTACs. It serves as an effective coupling agent, facilitating the conjugation of two molecules within PROTACs. This compound offers a stable and efficient platform for the delivery of targeted protein degradation therapeutics. [1]
T16053	Methylamino-PEG4-Boc	Methylamino-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.
T17050	Tetraethyl butane-1,4-diylbis(phosphoramidate)	Tetraethyl butane- 1, 4- diylbis(phosphoramid ate) is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1].
T17712	Cbz-aminooxy-PEG8-Boc	Cbz-aminooxy-PEG8-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.
T16589	Propargyl-PEG1-SS-PEG1-acid	Propargyl-PEG1-SS-PEG1-acid is a two-unit polyethylene glycol (PEG) linker that is cleavable and commonly employed in the synthesis of antibody-drug conjugates (ADCs) [1].
T18334	Methoxy-Tr-NH-PEG7	Methoxy-Tr-NH-PEG7 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.
T18119	m-PEG10-Br	m-PEG10-Br 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.
T14755	Boc-NH-PEG7-azide	Boc-NH-PEG7-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.
T14479	Azido-PEG8-NHS ester	Azido-PEG8-NHS ester is an 8 unit PEG linker with cleavable properties, commonly employed in the synthesis of antibody-drug conjugates (ADCs)[1]. This compound also serves as a PEG- and Alkyl/ether-based PROTAC linker, enabling its utilization in the synthesis of PROTACs[2].
T17887	cIAP1 Ligand-Linker Conjugates 15	cIAP1 Ligand-Linker Conjugates 15 consists of an IAP ligand that targets the E3 ubiquitin ligase, along with a PROTAC linker. This compound, cIAP1 Ligand-Linker Conjugates 15, is suitable for the development of SNIPERs[1].
T17152	Tr-PEG5-OH	Tr-PEG5-OH is a non-cleavable 5-unit PEG ADC linker utilized in the synthesis of antibody-drug conjugates (ADCs).
T17438	Amino-PEG6-amido-C16-COOH	Amino-PEG6-amido-C16-COOH, a PEG-based PROTAC linker, facilitates the synthesis of PROTACs[1].
T18152	m-PEG16-azide	m-PEG16-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.
T18365	Mp-polymer ester	Mp-polymer ester is a noncleavable antibody-drug conjugates (ADCs) linker typically employed in the synthesis of ADCs[1].
T14610	Biotin-PEG7-azide	Biotin-PEG7-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.

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PROTAC Linker