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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
T15924 m-PEG7-Ms m-PEG7-Ms is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
T17777 DBCO-PEG1-amine DBCO-PEG1-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.
T15977 Mal-PEG1-PFP ester Mal-PEG1-PFP ester, an alkyl/ether-based PROTAC linker, is utilized in PROTAC synthesis.
T17403 Amino-PEG10-CH2-Boc Amino-PEG10-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.
T17763 DBCO-NHCO-PEG2-amine DBCO-NHCO-PEG2-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.
T14006 Boc-NH-PEG4-CH2CH2COOH Boc-NH-PEG4-CH2CH2COOH is a PEG-based PROTAC linker employed in the synthesis of PROTAC[1]. Additionally, it is utilized as a cleavable ADC linker for antibody-drug conjugates (ADC)[2].
T17792 DBCO-PEG3-TCO DBCO-PEG3-TCO is a non-cleavable three-unit polyethylene glycol (PEG) linker employed for synthesizing antibody-drug conjugates (ADCs)[1].
T15952 Mal-amido-PEG2-TFP ester Mal-amido-PEG2-TFP ester is a polyethylene glycol (PEG)-based linker with amide functionality and trifluorophenyl (TFP) ester group. It finds application in PROTAC synthesis as a PEG-based PROTAC linker[1].
T15954 Mal-amido-PEG4-acid Mal-amido-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.
T16055 Methyltetrazine-acid Methyltetrazine-acid is an alkyl chain-derived linker employed for PROTAC synthesis[1].
T16235 N-(Mal-PEG6)-N-bis(PEG3-amine) N-(Mal-PEG6)-N-bis(PEG3-amine) is a Polyethylene Glycol (PEG)-based proteolysis targeting chimera (PROTAC) linker, which is utilized for the synthesis of PROTACs[1].
T17512 Azido-PEG36-Boc Azido-PEG36-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.
T16822 S-Acetyl-PEG3-C2-acid S-Acetyl-PEG3-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.
T16598 Propargyl-PEG2-amine Propargyl-PEG2-amine is a non-cleavable ADC linker employed for synthesizing antibody-drug conjugates (ADCs). It is a PEG-based PROTAC linker that finds applications in PROTAC synthesis [1][2].
T18250 MAL-di-EG-Val-Cit-PAB-MMAE MAL-di-EG-Val-Cit-PAB-MMAE comprises the linker MAL-di-EG-Val-Cit-PAB and the potent tubulin inhibitor MMAE, which are essential components of antibody-drug conjugates (ADCs).
T16916 SPDP-PEG4-acid SPDP-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.
T18160 m-PEG19-alcohol m-PEG19-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.
T15922 m-PEG7-CH2CH2CHO m-PEG7-CH2CH2CHO is a non-cleavable ADC linker utilized in the synthesis of antibody-drug conjugates (ADCs).
T16253 N3-PEG2-C2-NHS ester N3-PEG2-C2-NHS ester is a two-unit PEG linker, noncleavable in nature, specifically designed for the synthesis of antibody-drug conjugates (ADCs).
T18072 Lipoamide-PEG11-Mal Lipoamide-PEG11-Mal 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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