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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
T18854 Tos-PEG8-Tos Tos-PEG8-Tos 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.
T16918 SPDP-PEG6-NHS ester SPDP-PEG6-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.
T17474 Azide-PEG9-amido-C8-Boc Azide-PEG9-amido-C8-Boc is a polyethylene glycol (PEG) derived linker compound utilized for the synthesis of proteolysis-targeting chimeras (PROTACs)[1].
T18699 SNPB SNPB is a cleavable linker that is used for making antibody-drug conjugate (ADC).
T17812 DBCO-SS-amine DBCO-SS-amine is a cleavable linker vital in ADC synthesis. DBCO-SS-amine joins cytotoxic drugs to antibodies, enabling precise delivery to cells or proteins. The cleavable nature ensures controlled drug release, optimizing ADC effectiveness.
T16595 Propargyl-PEG10-Boc Propargyl-PEG10-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.
T16216 N-(Boc-PEG4)-NH-PEG4-NH-Boc N-(Boc-PEG4)-NH-PEG4-NH-Boc is a polyethylene glycol (PEG)-based PROteolysis TArgeting Chimera (PROTAC) linker, specifically designed for the synthesis of PROTACs [1].
T17704 Bromoacetamido-PEG9-ethylcarbamoyl-C8-Boc Bromoacetamido-PEG9-ethylcarbamoyl-C8-Boc represents a PEG-based PROTAC linker suitable for synthesizing PROTACs[1].
T16205 N-Boc-N-bis(PEG2-propargyl) N-Boc-N-bis(PEG2-propargyl) is a PEG-derived linker employed for synthesizing PROTACs[1].
T18285 Mal-PEG4-Glu(TFP ester)-NH-m-PEG24 Mal-PEG4-Glu(TFP ester)-NH-m-PEG24 is a polyethylene glycol (PEG)-based linker essential for the synthesis of proteolysis targeting chimeras (PROTACs)[1].
T16820 S-Acetyl-PEG3-azide S-Acetyl-PEG3-azide 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.
T14634 Bis-PEG3-acid Bis-PEG3-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.
T14533 Benzyl-PEG2-amine Benzyl-PEG2-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.
T17836 DMAC-SPP DMAC-SPP is a cleavable linker vital in ADC synthesis. DMAC-SPP joins cytotoxic drugs to antibodies, enabling precise delivery to cells or proteins. The cleavable nature ensures controlled drug release, optimizing ADC effectiveness.
T17648 Boc-C16-NHS ester Boc-C16-NHS ester, an alkyl/ether-based PROTAC linker, enables the synthesis of PROTACs[1].
T17796 DBCO-PEG4-Desthiobiotin DBCO-PEG4-Desthiobiotin is a polyethylene glycol (PEG) derivative utilized as a linker for the synthesis of proteolysis-targeting chimeras (PROTACs)[1].
T17732 CL2A CL2A is a pH-sensitive, cleavable PEG8- and triazole-containing PABC-peptide-mc linker, characterized by its ability to induce a bystander effect. It forms a disulfide bond with an antibody at a cysteine residue. Labetuzumab govitecan utilizes this linker for its drug conjugation[1].
T17416 Amino-PEG20-acid Amino-PEG20-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.
T17457 Azide-PEG-amine (MW 2000) Azide-PEG-amine (MW 2000) is a Polyethylene Glycol (PEG) derived linker compound utilized in the synthesis of Proteolysis Targeting Chimeras (PROTACs)[1].
T15913 m-PEG6-CH2CH2CHO m-PEG6-CH2CH2CHO is a non-cleavable ADC linker employed in the synthesis of antibody-drug conjugates (ADCs).
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