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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
T18767 TCO-PEG3-maleimide TCO-PEG3-maleimide is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
T17647 Boc-C1-PEG3-C4-OH Boc-C1-PEG3-C4-OH is an Alkyl/ether-based PROTAC linker utilized in the synthesis of PROTACs, which are characterized by their structure comprising two distinct ligands tethered by a linker. One ligand of PROTACs binds to an E3 ubiquitin ligase, while the other binds to the target protein. By leveraging the intracellular ubiquitin-proteasome system, PROTACs facilitate the targeted degradation of specific proteins[1].
T17339 (5,6)TAMRA-PEG3-Azide-PEG3-Desthiobiotin (5,6)TAMRA-PEG3-Azide-PEG3-Desthiobiotin is a polyethylene glycol (PEG)-based PROTAC linker utilized for the synthesis of PROTACs.
T17986 Gly-Gly-Gly-PEG3-TCO Gly-Gly-Gly-PEG3-TCO is a cleavable three-unit polyethylene glycol (PEG) linker employed in the synthesis of antibody-drug conjugates (ADCs)[1].
T16222 N-Bromoacetyl-β-alanine N-Bromoacetyl-β-alanine is an alkyl chain-derived PROTAC linker utilized for synthesizing PROTACs[1]. Moreover, it serves as a cleavable ADC linker in the production of antibody-drug conjugates (ADCs)[2].
T14789 Bromo-PEG2-C2-acid Bromo-PEG2-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.
T17124 Tos-PEG2-CH2COOH Tos-PEG2-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.
T17966 Fmoc-NH-PEG11-CH2COOH Fmoc-NH-PEG11-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.
T14624 Bis-Mal-Lysine-PEG4-TFP ester Bis-Mal-Lysine-PEG4-TFP ester, a PEG-based PROTAC linker, facilitates PROTAC synthesis[1].
T18273 Mal-PEG12-DSPE Mal-PEG12-DSPE 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.
T18626 Dox-Ph-PEG1-Cl Dox-Ph-PEG1-Cl, also referred to as PROTAC Linker 34, is a PEG-based compound employed for the synthesis of PROTACs[1].
T14713 Boc-Aminooxy-PEG3-azide Boc-Aminooxy-PEG3-azide is a polyethylene glycol (PEG) derived PROTAC linker, specifically designed for the synthesis of PROTACs[1].
T14277 Aminooxy-PEG7-methane Aminooxy-PEG7-methane 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.
T17709 Carboxymethyl-PEG-Carboxymethyl (MW 5000) Carboxymethyl-PEG-Carboxymethyl (MW 5000) is a polyethylene glycol (PEG)-based linker, specifically designed for the synthesis of PROTACs [1].
T15222 endo-BCN-PEG2-alcohol endo-BCN-PEG2-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.
T15315 Fmoc-NH-PEG2-CH2CH2COOH Fmoc-NH-PEG2-CH2CH2COOH is a cleavable ADC linker utilized in the synthesis of antibody-drug conjugates (ADCs)[1].
T18247 Mal-C2-Gly3-EDA Mal-C2-Gly3-EDA is a cleavable antibody-drug conjugate (ADC) linker equipped with a Maleimide moiety. It serves the purpose of facilitating the synthesis of ADCs.
T17502 Azido-PEG3-S-PEG3-azide Azido-PEG3-S-PEG3-azide is a polyethylene glycol (PEG)-derived linker specifically designed for the synthesis of proteolysis targeting chimeras (PROTACs)[1].
T17951 Fmoc-Gly-Gly-D-Phe-OtBu Fmoc-Gly-Gly-D-Phe-OtBu, an ADC cleavable linker, is utilized in the synthesis of antibody-drug conjugates. It is the R-isomer of Fmoc-Gly-Gly-Phe-OtBu [1].
T18458 N,N'-DME-N,N'-Bis-PEG2-acid N,N'-DME-N,N'-Bis-PEG2-acid is a polyethylene glycol (PEG)-derived linker used for the synthesis of proteolysis targeting chimeras (PROTACs)[1].
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