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
T17874	Nutlin carboxylic acid	Nutlin Carboxylic Acid (MDM2 ligand 1), derived from Nutlin 3, serves as an MDM2 ligand. It can be attached to a protein ligand via a linker to create PROTACs[1].
T16460	PEG4-sulfonic acid	PEG4-sulfonic 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.
T17685	Boc-NH-PEG9-propargyl	Boc-NH-PEG9-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.
T16631	Propargyl-PEG4-sulfonic acid	Propargyl-PEG4-sulfonic acid is a PEG4-based linker compound utilized in PROTAC synthesis[1].
T18077	m-PEG-acrylate (MW 10000)	m-PEG-acrylate (MW 10000) is a polyethylene glycol (PEG)-based linker utilized for the synthesis of Proteolysis Targeting Chimeras (PROTACs)[1].
T16309	NH-bis-PEG5	NH-bis-PEG5 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.
T14652	Bis-PEG9-NHS ester	Bis-PEG9-NHS ester, a cleavable ADC linker, is utilized in the synthesis of antibody-drug conjugates (ADCs)[1].
T14453	Azido-PEG4-Val-Cit-PAB-OH	Azido-PEG4-Val-Cit-PAB-OH is a 4-unit PEG ADC linker and a PEG-based PROTAC linker. It is employed for the synthesis of antibody-drug conjugates (ADCs)[1] and PROTACs[2].
T17089	THP-SS-PEG1-Tos	THP-SS-PEG1-Tos is a 1 unit PEG ADC linker that is cleavable. It is employed during the synthesis of antibody-drug conjugates (ADCs)[1].
T18389	N-(Biotin-PEG4)-N-bis(PEG4-acid)	N-(Biotin-PEG4)-N-bis(PEG4-acid) is a polyethylene glycol (PEG)-based linker molecule employed in the synthesis of PROTACs[1].
T17723	Cbz-NH-PEG36-C2-acid	Cbz-NH-PEG36-C2-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.
T17785	DBCO-PEG2-acid	DBCO-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.
T18069	Lenalidomide-propargyl-C2-amido-Ph-NH2 hydrochloride	Lenalidomide-propargyl-C2-amido-Ph-NH2 hydrochloride is a chemical compound that features a cereblon (CRBN) ligand, functioning as an E3 ubiquitin ligase, along with a linker. It can be utilized to create the PROTAC MD-224[1].
T14409	Azido-PEG1-methyl ester	Azido-PEG1-methyl ester is an alkyl/ether-based linker employed for the synthesis of PROTACs[1].
T18735	Sulfone-Bis-PEG4-acid	Sulfone-Bis-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.
T18772	TCO-PEG4-amine	TCO-PEG4-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.
T18383	N-(Azido-PEG3)-N-Fluorescein-PEG4-acid	N-(Azido-PEG3)-N-Fluorescein-PEG4-acid is a PEG-based PROTAC linker employed for the synthesis of PROTACs[1].
T15307	Fmoc-aminooxy-PEG4-acid	Fmoc-aminooxy-PEG4-acid is a PEG-based linker compound employed in the synthesis of PROTACs[1].
T17532	BCN-PEG3-VC-PFP ester	BCN-PEG3-VC-PFP ester is a three-unit PEG ADC linker that can be cleaved, and it is commonly employed in the synthesis of antibody-drug conjugates (ADCs) [1].
T17991	H2N-PEG4-Hydrazide	H2N-PEG4-Hydrazide 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