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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
T18128 m-PEG11-NHS ester m-PEG11-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.
T17855 DSPE-PEG13-TFP ester DSPE-PEG13-TFP 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.
T16202 N-Boc-diethanolamine N-Boc-diethanolamine is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
T15513 Hydroxy-PEG1-CH2-Boc Hydroxy-PEG1-CH2-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.
T18360 Methyltetrazine-Sulfo-NHS ester sodium Methyltetrazine-Sulfo-NHS ester (sodium) is an alkyl/ether-based PROTAC linker utilized for PROTAC synthesis[1].
T15883 m-PEG4-phosphonic acid ethyl ester m-PEG4-phosphonic acid ethyl ester is a PEGylation-based linker for the design and synthesis of PROTACs, which are heterobifunctional molecules facilitating targeted protein degradation[1].
T17572 Biotin-PEG24-TFP ester Biotin-PEG24-TFP 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.
T15988 Mal-PEG3-PFP ester Mal-PEG3-PFP 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.
T14825 Bromoacetamido-PEG4-NHS ester Bromoacetamido-PEG4-NHS ester is a PEGylated N-hydroxysuccinimide ester compound, specifically designed as a linker for PROTAC synthesis. This PEG-based PROTAC linker, when utilized, facilitates the creation of protein-targeted chimeras (PROTACs)[1].
T16593 Propargyl-PEG10-acid Propargyl-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.
T14697 BnO-PEG1-CH2COOH BnO-PEG1-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.
T17151 Tr-PEG4-OH Tr-PEG4-OH is a non-cleavable tetraethylene glycol ADC linker employed in ADC synthesis for the conjugation of antibodies and drugs.
T14645 Bis-PEG6-acid Bis-PEG6-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.
T14429 Azido-PEG3-maleimide Azido-PEG3-maleimide is a PEG-based PROTAC linker primarily used for the synthesis of PROTACs[1]. Additionally, it serves as a cleavable 3-unit PEG ADC linker employed in the synthesis of antibody-drug conjugates (ADCs)[2].
T14800 Bromo-PEG3-phosphonic acid diethyl ester Bromo-PEG3-phosphonic acid diethyl ester is a polyethylene glycol (PEG) derivative commonly employed as a linker for the assembly of proteolysis targeting chimeras (PROTACs)[1].
T18050 Iodo-PEG12-acid Iodo-PEG12-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.
T17662 Boc-NH-PEG10-CH2CH2NH2 Boc-NH-PEG10-CH2CH2NH2 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.
T18048 Hynic-PEG3-N3 Hynic-PEG3-N3 is a 3-unit PEG ADC linker, which is cleavable. It is commonly employed for the synthesis of antibody-drug conjugates (ADCs)[1].
T18567 Propargyl-PEG12-methane Propargyl-PEG12-methane is a polyethylene glycol (PEG)-based linker utilized in PROTAC synthesis, specifically for PEG-based proteolysis-targeting chimeras (PROTACs)[1].
T18406 N-Boc-PEG8-alcohol N-Boc-PEG8-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.
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