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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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. |