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 | |
---|---|---|
T16262 | N33-TEG-COOH | N33-TEG-COOH 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. |
T14540 | Benzyl-PEG5-azide | Benzyl-PEG5-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. |
T14576 | Biotin-C5-NHS Ester | Biotin-C5-NHS Ester is an alkyl/ether-based linker for PROTAC synthesis[1]. |
T18552 | Pomalidomide-amido-C1-Br | Pomalidomide-amido-C1-Br is a synthesized conjugate consisting of the Pomalidomide-based cereblon ligand and a linker, functioning as an E3 ligase ligand-linker. This compound serves as a tool for designing a B-Raf PROTAC degrader, specifically PROTAC B-Raf degrader 1, which exhibits anti-cancer activity[1]. |
T18401 | N-Boc-PEG23-bromide | N-Boc-PEG23-bromide 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. |
T14263 | Aminooxy-PEG3-acid | Aminooxy-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. |
T14024 | 3,4-Dibromo-Mal-PEG2-amine | 3,4-Dibromo-Mal-PEG2-amine is a polyethylene glycol (PEG) derivative and serves as a PEG-based PROTAC linker, facilitating the synthesis of PROTACs[1]. |
T14868 | Carboxy-PEG4-phosphonic acid | Carboxy-PEG4-phosphonic acid is a polyethylene glycol (PEG)-derived linker employed in the synthesis of Proteolysis Targeting Chimeras (PROTACs)[1]. |
T14276 | Aminooxy-PEG5-azide | Aminooxy-PEG5-azide is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs [1]. |
T18555 | Pomalidomide-PEG2-Tos | Pomalidomide-PEG2-Tos is a compound that consists of an E3 ligase ligand-linker conjugate. It is composed of a cereblon ligand conjugated to a two-unit PEG linker[1]. |
T16245 | N-(PEG3-acid)-N-bis(PEG3-amine) | N-(PEG3-acid)-N-bis(PEG3-amine) is a polyethylene glycol (PEG)-based linker utilized for the synthesis of proteolysis targeting chimeras (PROTACs)[1]. |
T15932 | m-PEG9-NHS ester | m-PEG8-CH2CH2-NHS ester is a PEG--based PROTAC linker can be used in the synthesis of PROTACs. |
T15937 | m-PEG8-succinimidyl carbonate | m-PEG8-succinimidyl carbonate is a polyethylene glycol (PEG)-derived linker, specifically designed for the synthesis of PROteolysis TArgeting Chimeras (PROTACs)[1]. |
T16823 | S-acetyl-PEG4-alcohol | S-acetyl-PEG4-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. |
T14820 | Bromoacetamido-PEG3-C2-acid | Bromoacetamido-PEG3-C2-acid is a polyethylene glycol (PEG) derived linker for the synthesis of proteolysis targeting chimeras (PROTACs)[1]. |
T18217 | m-PEG8-Boc | m-PEG8-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. |
T18683 | SMPT | SMPT, a non-cleavable ADC linker, is utilized in the production of antibody-drug conjugates (ADCs). |
T18218 | m-PEG8-DBCO | m-PEG8-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. |
T15894 | m-PEG5-Ms | m-PEG5-Ms is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1]. |
T18051 | Iodo-PEG12-NHS ester | Iodo-PEG12-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. |