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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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]. |