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
T17985	Gemcitabine-O-Si(di-iso)-O-Mc	Gemcitabine-O-Si(di-iso)-O-Mc, a drug-linker conjugate for Antibody-Drug Conjugates (ADC), exhibits potent antitumor activity. It incorporates Gemcitabine, a pyrimidine nucleoside analog antimetabolite and antineoplastic agent, connected through the ADC linker[1].
T17661	Boc-NH-PEG10-CH2CH2COOH	Boc-NH-PEG10-CH2CH2COOH is a polyethylene glycol (PEG)-based PROTAC linker utilized for PROTAC synthesis[1].
T16261	N3-PEG8-CH2COOH	N3-PEG8-CH2COOH 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.
T17494	Azido-PEG20-alcohol	Azido-PEG20-alcohol 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.
T18527	PDdB-Pfp	PDdB-Pfp is a reducible ADC (antibody-drug conjugate) linker designed for agents targeting the extracellular loop 1 (ECL1) of TM4SF1 (transmembrane 4 L6 family member 1).
T18286	Mal-PEG4-Lys(t-Boc)-NH-m-PEG24	Mal-PEG4-Lys(t-Boc)-NH-m-PEG24 is a polyethylene glycol (PEG)-based PROTAC linker, suitable for the synthesis of PROTACs[1].
T16461	PEG5-bis-(Ethyl phosphonate)	PEG5-bis-(Ethyl phosphonate) is a polyethylene glycol (PEG) derived PROTAC linker employed for PROTAC synthesis[1].
T16238	N-Methyl-N-(t-Boc)-PEG4-acid	N-Methyl-N-(t-Boc)-PEG4-acid is a polyethylene glycol (PEG) derivative utilized as a PROTAC linker in the synthesis of PROTACs, which refers to proteolysis-targeting chimeras[1].
T14255	Amino-PEG9-Boc	Amino-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.
T17605	Bis-Mal-PEG5	Bis-Mal-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.
T17555	Biotin-PEG-triethoxysilane (MW 5000)	Biotin-PEG-triethoxysilane (MW 5000) is a PEG-based PROTAC linker utilized for PROTAC synthesis[1].
T15511	Hydroxy-PEG1-C2-methyl ester	Hydroxy-PEG1-C2-methyl ester is a polyethylene glycol (PEG) derived linker widely employed for the production of PROTACs - proteolysis targeting chimeras. [1]
T15888	m-PEG5-acid	m-PEG5-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.
T13989	1,1,1-Trifluoroethyl-PEG4-Tos	1,1,1-Trifluoroethyl-PEG4-Tos is a polyethylene glycol (PEG) derived linker molecule which offers utility in the synthesis of Proteolysis Targeting Chimeras (PROTACs)[1].
T14625	Bis-Mal-PEG3	Bis-Mal-PEG3 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.
T18624	NH2-Ph-C4-acid-NH2-Me	NH2-Ph-C4-acid-NH2-Me (PROTAC Linker 31) is an alkyl chain-based compound utilized for the synthesis of PROTACs. [1]
T17525	Azidoethyl-SS-propionic NHS ester	Azidoethyl-SS-propionic NHS ester is a cleavable linker frequently employed in the synthesis of antibody-drug conjugates (ADCs) [1].
T14749	Boc-NH-PEG5-propargyl	Boc-NH-PEG5-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.
T14757	Boc-NH-PEG7-propargyl	Boc-NH-PEG7-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.
T14742	Boc-NH-PEG3-propargyl	Boc-NH-PEG3-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.

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PROTAC Linker