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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
T18287 Mal-PEG4-Lys(TFA)-NH-m-PEG24 Mal-PEG4-Lys(TFA)-NH-m-PEG24 is a polyethylene glycol (PEG) derivative specifically designed as a PROTAC linker for the synthesis of proteolysis targeting chimeras (PROTACs) [1].
T15879 m-PEG4-Hydrazide m-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.
T17437 Amino-PEG6-amido-C16-Boc Amino-PEG6-amido-C16-Boc is a PEG-based PROTAC linker employed for the synthesis of PROTACs[1].
T18364 Tesirine MP-PEG8-VA-PABC-PBD Dimer is a drug-linker conjugates for ADC which is used in the treatment of several cancers. PBD Dimer is a DNA alkylating which inhibits DNA replication[1].
T17358 Acrylate-PEG-NH2 (MW 10000) Acrylate-PEG-NH2 (MW 10000) is a polyethylene glycol (PEG)-based linker utilized in the synthesis of PROTACs[1].
T14706 Boc-Aminooxy-PEG1-azide Boc-Aminooxy-PEG1-azide is a polyethylene glycol (PEG) derived linker compound designed specifically for the synthesis of proteolysis targeting chimeras (PROTACs)[1].
T14804 Bromo-PEG5-alcohol Bromo-PEG5-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.
T14225 Amino-PEG10-OH Amino-PEG10-OH is a non-cleavable 10-unit PEG ADC linker employed in the synthesis of antibody-drug conjugates (ADCs)[1].
T14663 Bis-Tos-(2-hydroxyethyl disulfide) Bis-Tos-(2-hydroxyethyl disulfide) is a cleavable linker employed in the synthesis of antibody-drug conjugates (ADCs)[1].
T15298 Fluorescein-thiourea-PEG4-azide Fluorescein-thiourea-PEG4-azide, a PEG-based PROTAC linker, is employed for the synthesis of PROTACs.
T15517 Hydroxy-PEG2-C2-PFP ester Hydroxy-PEG2-C2-PFP ester, a PEG/Alkyl/ether-based PROteolysis TArgeting Chimeric (PROTAC) linker, is suitable for the synthesis of PROTACs.
T18189 m-PEG3-Sulfone-PEG4-propargyl m-PEG3-Sulfone-PEG4-propargyl is a polyethylene glycol (PEG)-based prodrug-induced degradation (PROTAC) linker. It is utilized in the efficient synthesis of PROTACs, a class of heterobifunctional molecules designed to selectively target and degrade specific protein targets[1].
T16312 NH2-PEG3 NH2-PEG3 (PROTAC Linker 35) is a polyethylene glycol (PEG) linker utilized in the synthesis of PROTAC (β-NF-JQ1)[1].
T14165 Ald-Ph-amido-PEG4-C2-NHS ester Ald-Ph-amido-PEG4-C2-NHS ester is a non-cleavable 4-unit PEG linker employed in antibody-drug conjugation (ADC) to connect antibodies with drugs.
T16184 N-(Azido-PEG3)-N-Biotin-PEG4-methyl ester N-(Azido-PEG3)-N-Biotin-PEG4-methyl ester is a polyethylene glycol (PEG) derivative used as a PROTAC linker for the synthesis of Proteolysis Targeting Chimeras (PROTACs)[1].
T18463 NHS-C4-MTS N-Succinimidyloxycarbonylpropyl methanethiosulfonate (SMPM) is a non-cleavable antibody-drug conjugate (ADC) linker employed for ADC synthesis[1].
T17830 Dioxoisoindolin-O-PEG-OH (MW 2000) Dioxoisoindolin-O-PEG-OH (MW 2000) is a polyethylene glycol (PEG)-based linker utilized for the synthesis of PROTACs (proteolysis targeting chimeras)[1].
T17318 1,1,1-Trifluoroethyl-PEG4-propargyl 1,1,1-Trifluoroethyl-PEG4-propargyl is a polyethylene glycol (PEG)-based PROTAC linker employed for the synthesis of PROTACs [1].
T14430 Azido-PEG3-methyl ester Azido-PEG3-methyl ester is a polyethylene glycol (PEG)-derived linker employed for the synthesis of proteolysis-targeting chimeras (PROTACs)[1].
T18796 Tetrazine-Ph-NHCO-PEG4-alkyne Tetrazine-Ph-NHCO-PEG4-alkyne is a PEG4-based linker for PROTACs synthesis[1].
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