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 | |
---|---|---|
T17902 | Nutlin-C1-amido-PEG4-C2-N3 | Nutlin-C1-amido-PEG4-C2-N3 is a novel compound that functions as a ligand-linker conjugate for the E3 ligase. It is a synthesized molecule incorporating the MDM2 ligand derived from Nutlin 3, and a 4-unit PEG linker. This compound is specifically designed for utilization in PROTAC technology. |
T17947 | Fmoc-aminooxy-PEG12-acid | Fmoc-aminooxy-PEG12-acid, a PEG-based PROTAC linker, is employed for synthesizing PROTACs[1]. |
T18779 | TCO-PEG8-acid | TCO-PEG8-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. |
T18380 | N-(Azido-PEG3)-N-bis(PEG4-Boc) | N-(Azido-PEG3)-N-bis(PEG4-Boc) is a polyethylene glycol (PEG) derivative specifically designed as a linker for PROteolysis TArgeting Chimeras (PROTACs)[1]. |
T18263 | Mal-PEG-mal (MW 2000) | Mal-PEG-mal (MW 2000) 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. |
T18875 | (Ac)Phe-Lys(Alloc)-PABC-PNP | '(Ac)Phe-Lys(Alloc)-PABC-PNP serves as a valuable cleavable linker in the development of antibody-drug conjugates.' |
T15985 | Mal-PEG3-alcohol | Mal-PEG3-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. |
T18399 | N-Boc-PEG16-alcohol | N-Boc-PEG16-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. |
T14023 | 3-(2-Pyridyldithio)propanoic Acid | 3-(2-Pyridyldithio)propanoic Acid is an alkyl chain-derived PROTAC linker applicable for synthesizing PROTACs[1]. |
T15224 | endo-BCN-PEG3-acid | endo-BCN-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. |
T14892 | Cbz-NH-PEG8-C2-acid | Cbz-NH-PEG8-C2-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. |
T18362 | Vc-seco-DUBA | Vc-seco-DUBA is a drug-linker conjugate for ADC with potent antitumor activity by using DUBA (DNA alkylating agent), linked via the ADC linker Vc-seco[1]. |
T18081 | m-PEG-Aminooxy (MW 2000) | m-PEG-Aminooxy (MW 2000) is a polyethylene glycol (PEG) derived PROTAC linker, primarily utilized for the synthesis of proteolysis-targeting chimeras (PROTACs)[1]. |
T18417 | N-Hydroxypropyl-N'-(azide-PEG3)-Cy3 | N-Hydroxypropyl-N’-(azide-PEG3)-Cy3 is a polyethylene glycol (PEG)-based linker specifically designed for use in the synthesis of proteolysis targeting chimeras (PROTACs)[1]. |
T17062 | Tetrazine-Ph-NHS ester | Tetrazine-Ph-NHS ester is an alkyl/ether-based PROTAC linker commonly employed for synthesizing PROTACs[1]. |
T18676 | (S)-TCO-PEG3-amine | (S)-TCO-PEG3-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. |
T14709 | Boc-Aminooxy-PEG2-C2-amine | Boc-Aminooxy-PEG2-C2-amine is a polyethylene glycol (PEG)-based linker molecule, intended for use in the synthesis of proteolysis-targeting chimeras (PROTACs)[1]. |
T15121 | Diethyl 12-bromododecylphosphonate | Diethyl 12-bromododecylphosphonate is an alkyl chain-derived PROTAC linker employed for the synthesis of PROTACs[1]. |
T18800 | Tetrazine-Ph-PEG4-Ph-aldehyde | Tetrazine-Ph-PEG4-Ph-aldehyde is a polyethylene glycol (PEG) derived linker, specifically designed for the synthesis of proteolysis-targeting chimeras (PROTACs)[1]. |
T17851 | DSPE-PEG-CH2COOH (MW 2000) | DSPE-PEG-CH2COOH (MW 2000) is a polyethylene glycol (PEG)-based linker molecule. It is specifically designed for the synthesis of protein-targeting chimeras (PROTACs)[1]. |