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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
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].
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