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
T15851	m-PEG3-Amine	m-PEG3-Amine is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
T18403	N-(Boc-PEG3)-N-bis(PEG3-acid)	N-(Boc-PEG3)-N-bis(PEG3-acid) is a polyethylene glycol (PEG)-based linker compound utilized for the synthesis of proteolysis-targeting chimeras (PROTACs)[1].
T14396	Azide-PEG5-Boc	Azide-PEG5-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.
T17624	Bis-PEG21-NHS ester	Bis-PEG21-NHS ester is a cleavable ADC linker utilized in the synthesis of antibody-drug conjugates (ADCs) [1].
T14737	Boc-NH-PEG2-CH2CH2COOH	Boc-NH-PEG2-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.
T14100	Acid-PEG2-SS-PEG2-acid	Acid-PEG2-SS-PEG2-acid is a 4-unit PEG ADC linker that employs cleavable bonds. It is utilized in the synthesis of antibody-drug conjugates (ADCs)[1].
T15865	m-PEG3-succinimidyl carbonate	m-PEG3-succinimidyl carbonate is a polyethylene glycol (PEG)-based linker, specifically designed for the synthesis of proteolysis-targeting chimeras (PROTACs)[1].
T18246	Mal-C2-Gly3-EDA-PNU-159682	Mal-C2-Gly3-EDA-PNU-159682, a drug-linker conjugate for antibody-drug conjugates (ADC), combines the cleavable ADC linker Mal-C2-Gly3-EDA with the potent ADC cytotoxin PNU-159682.
T18390	N-(Biotin-PEG4)-N-bis(PEG4-Boc)	N-(Biotin-PEG4)-N-bis(PEG4-Boc) is a polyethylene glycol (PEG)-based linker utilized for the synthesis of proteolysis-targeting chimeras (PROTACs)[1].
T14016	2-Hydroxyethyl disulfide mono-tosylate	2-Hydroxyethyl disulfide mono-tosylate is a cleavable linker compound employed in the synthesis of antibody-drug conjugates (ADCs)[1].
T18335	Methylcyclopropene-PEG3-amine	Methylcyclopropene-PEG3-amine is a cleavable three-unit polyethylene glycol (PEG) linker employed in the synthesis of antibody-drug conjugates (ADCs)[1].
T15062	DBCO-NHCO-PEG4-amine	DBCO-NHCO-PEG4-amine is a cleavable ADC linker used to conjugate MMAE and antibody (e.g., DBCO-VCpAB MMAE and DBCO-TRX MMAE with EC50s of 280 nM and 22 nM in SKBR3 cells, respectively) [1].
T18538	MAC glucuronide phenol-linked SN-38	MAC glucuronide phenol-linked SN-38, a pH-sensitive lactone and DNA topoisomerase I inhibitor drug linker, exhibits cytotoxicity in L540cy and Ramos cells, with IC50 values of 113 ng/mL and 67 ng/mL, respectively[1].
T18238	Mal-amido-PEG12-TFP ester	Mal-amido-PEG12-TFP ester is a polyethylene glycol (PEG)-based linker utilized for the synthesis of proteolysis targeting chimeras (PROTACs)[1].
T18738	t-Boc-Aminooxy-PEG12-acid	t-Boc-Aminooxy-PEG12-acid is a polyethylene glycol (PEG)-based PROTAC linker, utilized for synthesizing PROTACs[1].
T15841	m-PEG2-acid	m-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.
T14407	Azido-PEG1-CH2CO2-NHS	Azido-PEG1-CH2CO2-NHS is an alkyl/ether-based linker used for the synthesis of PROTACs[1].
T17508	Azido-PEG3-Sulfone-PEG4-Boc	Azido-PEG3-Sulfone-PEG4-Boc is a polyethylene glycol (PEG)-based PROTAC linker, utilized for the synthesis of PROTACs[1].
T18411	N-(DBCO-PEG4)-N-Biotin-PEG4-NHS	N-(DBCO-PEG4)-N-Biotin-PEG4-NHS is a PEG-based PROTAC linker suitable for synthesizing PROTACs[1].
T17417	Amino-PEG20-Boc	Amino-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.

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PROTAC Linker