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 | |
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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. |