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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
T17443 Amino-SS-PEG12-acid Amino-SS-PEG12-acid, a cleavable 12-unit polyethylene glycol (PEG) linker, is commonly used in the synthesis of antibody-drug conjugates (ADCs)[1].
T17788 DBCO-(PEG2-Val-Cit-PAB)2 DBCO-(PEG2-Val-Cit-PAB)2 is a dual-cleavable linker used in antibody-drug conjugates (ADCs).
T17527 BCN-PEG1-Val-Cit-OH BCN-PEG1-Val-Cit-OH is a cleavable one-unit polyethylene glycol (PEG) linker employed in the synthesis of antibody-drug conjugates (ADCs) [1].
T14517 BDP FL-PEG4-amine BDP FL-PEG4-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.
T17840 DNP-PEG6-acid DNP-PEG6-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.
T16054 Methylamino-PEG5-azide Methylamino-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.
T18421 N-(m-PEG4)-N'-(Acid-PEG3)-benzothiazole Cy5 N-(m-PEG4)-N'-(Acid-PEG3)-benzothiazole Cy5 is a polyethylene glycol-based linker termed PEG-PROTAC, suitable for the development of PROTACs through chemical synthesis[1].
T18090 m-PEG-Lys-NHS ester (MW 20000) m-PEG-Lys-NHS ester (MW 20000) is an alkyl/ether-based PROTAC linker commonly employed in PROTAC synthesis[1].
T14824 Bromoacetamido-PEG4-C2-Boc Bromoacetamido-PEG4-C2-Boc is a polyethylene glycol (PEG)- and alkyl/ether-based linker commonly employed for the synthesis of proteolysis targeting chimeras (PROTACs)[1].
T18579 Propargyl-PEG3-methyl ester Propargyl-PEG3-methyl ester is a propargyl polyethylene glycol (PEG) derivative that serves as a linker in the synthesis of proteolysis-targeting chimeras (PROTACs)[1].
T14452 Azido-PEG4-tetra-Ac-beta-D-glucose Azido-PEG4-tetra-Ac-beta-D-glucose is a polyethylene glycol (PEG) based PROTAC linker utilized for the synthesis of PROTACs[1].
T17423 Amino-PEG24-CH2-Boc Amino-PEG24-CH2-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.
T15190 (S,R,S)-AHPC-PEG4-NH2 hydrochloride (S, R, S)-AHPC-PEG4-NH2 hydrochloride is a chemically synthesized conjugate consisting of an E3 ligase ligand-linker, incorporating the VHL ligand based on (S, R, S)-AHPC, and a 4-unit PEG linker, which are specifically designed for use in PROTAC technology.
T14258 Aminoethyl-SS-propionic acid Aminoethyl-SS-propionic acid is an ADC linker compound employed in ADC synthesis [1]. It functions as a cleavable linker in the conjugation of antibodies with drugs, allowing for targeted drug delivery.
T18366 Ms-PEG10-t-butyl ester Ms-PEG10-t-butyl 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.
T18438 N-(m-PEG9)-N'-(PEG5-acid)-Cy5 N-(m-PEG9)-N'-(PEG5-acid)-Cy5 is a PEG-based PROTAC linker employed for the synthesis of PROTACs[1].
T17971 Fmoc-NH-PEG25-CH2CH2COOH Fmoc-NH-PEG25-CH2CH2COOH, a PEG-based PROTAC linker, facilitates the synthesis of PROTACs[1].
T18019 HS-C6-PEG9-acid HS-C6-PEG9-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.
T17808 DBCO-PEG9-amine DBCO-PEG9-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.
T18876 β-Estradiol-6-CMO-PEG3-biotin β-Estradiol-6-CMO-PEG3-biotin serves as a cleavable 3-unit PEG ADC linker for the synthesis of antibody-drug conjugates (ADCs)[1].
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