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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
T18575 Propargyl-PEG2-beta-D-glucose Propargyl-PEG2-beta-D-glucose is a polyethylene glycol (PEG) derived linker compound specifically designed for the synthesis of proteolysis targeting chimeras (PROTACs)[1].
T18418 N-(Iodoacetamido)-Doxorubicin N-(Iodoacetamido)-Doxorubicin is an ADC linker employed in the synthesis of antibody-drug conjugates (ADCs)[1].
T18573 Propargyl-PEG14-Boc Propargyl-PEG14-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.
T18859 Tri(Mal-PEG2-amide)-amine Tri(Mal-PEG2-amide)-amine is a polyethylene glycol (PEG)-derived linker commonly employed for synthesizing proteolysis-targeting chimeras (PROTACs)[1].
T14416 Azido-PEG2-alcohol Azido-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.
T17894 cIAP1 Ligand-Linker Conjugates 3 cIAP1 Ligand-Linker Conjugates 3 are chemical compounds comprising an IAP ligand designed specifically for the E3 ubiquitin ligase and a PROTAC linker. These conjugates, denoted as cIAP1 Ligand-Linker Conjugates 3, find utility in the design of SNIPERs, short for Specific and Non-genetic IAP-dependent Protein Erasers [1].
T17625 Bis-PEG23-endo-BCN Bis-PEG23-endo-BCN 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.
T17856 DSPE-PEG36-DBCO DSPE-PEG36-DBCO 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.
T18847 THP-PEG4-Pyrrolidine(N-Me)-CH2OH THP-PEG4-Pyrrolidine(N-Me)-CH2OH, a PEG-based PROTAC linker, facilitates the synthesis of PROTAC K-Ras Degrader-1[1].
T18201 m-PEG4-phosphonic acid m-PEG4-phosphonic 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.
T14611 Biotin-PEG8-alcohol Biotin-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.
T17729 Cl-C6-PEG4-C3-COOH Cl-C6-PEG4-C3-COOH, a PROTAC linker, is a suitable component for synthesizing chloroalkane-containing PROTACs (HaloPROTACs).
T18698 SNPB-sulfo-Me SNPB-sulfo-Me is a cleavable linker used in the development of antibody-drug conjugates (ADC).
T18186 m-PEG3-Sulfone-PEG3-azide m-PEG3-Sulfone-PEG3-azide is a polyethylene glycol (PEG)-based linker widely employed in the synthesis of PROTACs, which stands for Proteolysis Targeting Chimeras[1].
T17660 Boc-NH-PEG1-Ph-O-CH2COOH Boc-NH-PEG1-Ph-O-CH2COOH is a PROTAC linker used for the EED-targeted PROTAC [1].
T14460 Azido-PEG5-CH2CO2-PFP Azido-PEG5-CH2CO2-PFP is a polyethylene glycol (PEG) and Alkyl/ether-based linker compound. It serves as a key component in the synthesis of proteolysis-targeting chimeras (PROTACs), a class of molecules used for targeted protein degradation[1].
T15990 Mal-PEG4-Boc Mal-PEG4-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.
T18533 PEG3-C4-OBn PEG3-C4-OBn, a polyethylene glycol (PEG)-based PROTAC linker, is utilized in crafting the PROTAC SGK3 degrader-1, a potent SKG3 degrader leveraging PROTAC technology [1][2].
T18559 PPC-NHS ester PPC-NHS ester is a cleavable linker vital in ADC synthesis. PPC-NHS ester joins cytotoxic drugs to antibodies, enabling precise delivery to cells or proteins. The cleavable nature ensures controlled drug release, optimizing ADC effectiveness.
T15895 m-PEG5-NH2 m-PEG5-NH2 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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