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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
T16234 N-Mal-N-bis(PEG4-NHS ester) N-Mal-N-bis(PEG4-NHS ester) is a polyethylene glycol (PEG)-based bifunctional linker utilized for synthesizing Proteolysis Targeting Chimeras (PROTACs)[1].
T17061 Tetrazine-Ph-acid Tetrazine-Ph-acid is an alkyl chain-derived PROTAC linker employed in PROTAC synthesis[1].
T16313 NH2-PEG4-CH2CH2COOH NH2-PEG4-CH2CH2COOH is a cleavable 4-unit PEG linker utilized in the synthesis of antibody-drug conjugates (ADCs).
T14851 C2-Bis-phosphoramidic acid diethyl ester C2-Bis-phosphoramidic acid diethyl ester is an alkyl chain-derived PROTAC linker utilized for the synthesis of PROTACs[1].
T14241 Amino-PEG4-CH2COOH Amino-PEG4-CH2COOH is a PEG-based PROTAC linker and a non-cleavable 4 unit PEG ADC linker employed in the synthesis of PROTACs and antibody-drug conjugates (ADCs).
T18372 N-(Amino-PEG3)-N-bis(PEG4-Boc) N-(Amino-PEG3)-N-bis(PEG4-Boc) is a polyethylene glycol (PEG) derivative commonly employed as a linker in the creation of proteolysis targeting chimeras (PROTACs)[1].
T15223 endo-BCN-PEG2-PFP ester Endo-BCN-PEG2-PFP ester, a PEG-based linker, serves as a valuable component in PROTAC synthesis[1].
T18646 Pyrene-PEG5-biotin Pyrene-PEG5-biotin 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.
T17757 DBCO-NHCO-C4-NHS ester DBCO-NHCO-C4-NHS ester is an alkyl chain-derived PROTAC linker applicable for PROTACs synthesis[1].
T17725 Cbz-NH-PEG8-CH2COOH Cbz-NH-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.
T17459 Azide-PEG-amine (MW 5000) Azide-PEG-amine (MW 5000) is a polyethylene glycol (PEG)-derived linker compound with azide functionality, primarily utilized in the synthesis of proteolysis-targeting chimeras (PROTACs)[1].
T17075 Thiol-PEG3-Boc Thiol-PEG3-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.
T14474 Azido-PEG8-amine Azido-PEG8-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.
T17085 THP-PEG8-OH THP-PEG8-OH 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.
T14739 Boc-NH-PEG2-NH-Boc Boc-NH-PEG2-NH-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.
T17997 HO-PEG-amine (MW 1000) HO-PEG-amine (MW 1000) 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.
T18344 Methyltetrazine-PEG24-Boc Methyltetrazine-PEG24-Boc is a polyethylene glycol (PEG) derivative utilized as a linker compound in PROTAC synthesis. This PEG-based linker enables the construction of PROTACs[1].
T18044 Hydroxy-PEG4-C2-nitrile Hydroxy-PEG4-C2-nitrile is a polyethylene glycol (PEG) based linker commonly employed in the synthesis of Proteolysis Targeting Chimeras (PROTACs)[1].
T18409 N-DBCO-N-bis(PEG2-C2-acid) N-DBCO-N-bis(PEG2-C2-acid) is a polyethylene glycol (PEG) linker commonly employed in the synthesis of proteolysis-targeting chimeras (PROTACs)[1].
T18704 SPDH SPDH is a cleavable antibody-drug conjugate (ADC) linker utilized for the diagnosis and therapy of cancer as well as B cell proliferative diseases.
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