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
T15305	Fmoc-amino-PEG3-CH2COOH	Fmoc-amino-PEG3-CH2COOH is a polyethylene glycol (PEG)-based linker, primarily employed for the synthesis of proteolysis-targeting chimeras (PROTACs)[1].
T15914	m-PEG6-CH2CH2COOH	m-PEG6-CH2CH2COOH 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.
T17354	Acid-PEG25-NHS ester	Acid-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.
T17645	Boc-aminoxy-PEG4-acid	Boc-aminoxy-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.
T17735	Cy5-PEG4-acid	Cy5-PEG4-acid (chloride) serves as a PEG-based PROTAC linker, suitable for synthesizing PROTACs[1].
T14469	Azido-PEG6-C2-Boc	Azido-PEG6-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.
T14468	Azido-PEG6-C1-Boc	Azido-PEG6-C1-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.
T18801	Tetrazine-Ph-PEG5-Ph-tetrazine	Tetrazine-Ph-PEG5-Ph-tetrazine is a PEG-based PROTAC linker utilized for the synthesis of PROTACs[1].
T15064	DBCO-NHCO-PEG4-NHS ester	DBCO-NHCO-PEG4-NHS ester ester is a MMP-2- and cathepsin B- (CatB) cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
T16295	NH-bis(C2-PEG1-azide)	NH-bis(C2-PEG1-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.
T16177	N-(Azido-PEG2)-N-Boc-PEG3-acid	N-(Azido-PEG2)-N-Boc-PEG3-acid is a polyethylene glycol (PEG) derived linker compound, specifically designed for PROTAC synthesis[1].
T14260	Aminooxy-PEG1-propargyl	Aminooxy-PEG1-propargyl 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.
T18221	m-PEG8-ethoxycarbonyl-propanoic acid	m-PEG8-ethoxycarbonyl-propanoic acid, a PEG-derived PROTAC linker, is employed for the synthesis of PROTACs[1].
T18451	N-methyl-N'-methyl-O-(m-PEG4)-O'-(propargyl-PEG4)-Cy5	N-methyl-N'-methyl-O-(m-PEG4)-O'-(propargyl-PEG4)-Cy5 is a polyethylene glycol (PEG)-based linker commonly employed in the synthesis of proteolysis-targeting chimeras (PROTACs)[1].
T15968	Mal-C6-amine TFA	Mal-C6-amine (TFA) is an alkyl chain-based linker employed in the synthesis of PROTACs[1].
T15311	Fmoc-NH-ethyl-SS-propionic acid	Fmoc-NH-ethyl-SS-propionic acid is a cleavable linker compound utilized for the synthesis of antibody-drug conjugates (ADCs)[1].
T15071	DBCO-PEG4-DBCO	DBCO-PEG4-DBCO is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
T16258	N3-PEG3-CH2CH2COOH	N3-PEG3-CH2CH2COOH, a PEG-based PROTAC linker, is utilized in the synthesis of BI-3663, BI-4216, and BI-0319. Additionally, Azido-PEG3-acid, a non-cleavable 3-unit PEG ADC linker, is employed in the synthesis of antibody-drug conjugates (ADCs).
T16644	Propargyl-PEG7-acid	Propargyl-PEG7-acid is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
T14588	Biotin-PEG2-NHS ester	Biotin-PEG2-NHS ester 是一种 PROTAC linker，由生物素、PEG和NHS组成，可用于合成 PROTAC 。

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PROTAC Linker