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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
T17077 Thiol-PEG4-acid Thiol-PEG4-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.
T17819 Thalidomide-O-amido-C8-NH2 Thalidomide-O-amido-C8-NH2 (Cereblon Ligand-Linker Conjugates 2) is a synthesized E3 ligase ligand-linker conjugate comprising a Thalidomide-based cereblon ligand and a linker. This compound is useful in the synthesis of PROTACs, as per reference [1].
T18208 m-PEG49-NHS ester m-PEG49-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.
T14793 Bromo-PEG2-phosphonic acid diethyl ester Bromo-PEG2-phosphonic acid diethyl ester is a polyethylene glycol (PEG)-based linker used in the synthesis of proteolysis targeting chimeras (PROTACs)[1].
T18260 Mal-NH-PEG6-CH2CH2COOPFP ester Mal-NH-PEG6-CH2CH2COOPFP ester is a polyethylene glycol (PEG)-based linker known as a PROTAC linker, designed specifically for the synthesis of PROTACs[1].
T18521 PC DBCO-PEG3-biotin PC DBCO-PEG3-biotin is a trimeric polyethylene glycol (PEG) linker, specifically designed for antibody-drug conjugate (ADC) synthesis, with a cleavable moiety consisting of a dibenzocyclooctyne (DBCO) group and a biotin molecule. This linker provides a platform for the efficient attachment of drugs to antibodies, facilitating the targeted delivery and controlled release of therapeutic agents in ADCs[1].
T17466 Azide-PEG16-alcohol Azide-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.
T16307 NH-bis(PEG4-C2-NH-Boc) NH-bis(PEG4-C2-NH-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.
T17690 Boc-Val-Ala-PAB-PNP Boc-Val-Ala-PAB-PNP is an ADC linker employed for the synthesis of antibody-drug conjugates (ADCs)[1]. This cleavable compound efficiently facilitates the attachment of drugs to antibodies, allowing for targeted delivery and release of therapeutic agents within the body, making it an important component in ADC development.
T17816 DBCO-Val-Cit-PABC-PNP DBCO-Val-Cit-PABC-PNP is a cleavable linker for antibody-drug conjugate (ADC) synthesis[1].
T16182 N-(Azido-PEG2)-N-Boc-PEG4-NHS ester N-(Azido-PEG2)-N-Boc-PEG4-NHS ester, a PEG-based PROTAC linker, facilitates the synthesis of PROTACs[1].
T17869 cIAP1 ligand 2 cIAP1 ligand 2, a derivative of LCL161, is an IAP ligand that can be connected to the ABL ligand for protein via a linker, resulting in the formation of SNIPER.
T18753 TCO-PEG1-Val-Cit-OH TCO-PEG1-Val-Cit-OH is a cleavable 1-unit polyethylene glycol (PEG) linker utilized in the synthesis of antibody-drug conjugates (ADCs)[1].
T14772 Br-PEG4-CH2-Boc Br-PEG4-CH2-Boc, a PEG- and Alkyl/ether-based PROTAC linker, serves as a valuable component for the synthesis of PROTACs[1].
T17984 Folate-PEG3-azide Folate-PEG3-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.
T18434 N-(m-PEG4)-N'-(PEG2-NHS ester)-Cy5 N-(m-PEG4)-N'-(PEG2-NHS ester)-Cy5 is a polyethylene glycol (PEG) based PROTAC linker utilized for the synthesis of PROTACs[1].
T17592 Biotin-PEG6-Thalidomide Biotin-PEG6-Thalidomide 是一种基于 PEG 的 PROTAC linker。
T14027 3,4-Dibromo-Mal-PEG8-Boc 3,4-Dibromo-Mal-PEG8-Boc is a polyethylene glycol (PEG) derived PROTAC linker utilized in PROTAC synthesis[1].
T18196 m-PEG37-acid m-PEG37-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.
T17078 Thiol-PEG4-Boc Thiol-PEG4-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.
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