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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T15321 | Fmoc-NH-PEG6-CH2COOH | Fmoc-NH-PEG6-CH2COOH is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs) [1]. |
T17772 | DBCO-NHCO-PEG6-maleimide | DBCO-NHCO-PEG6-maleimide is a polyethylene glycol (PEG)-based linker compound employed in the synthesis of proteolysis-targeting chimeras (PROTACs)[1]. |
T14157 | Ald-CH2-PEG4-Boc | Ald-CH2-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. |
T14700 | BnO-PEG5-Boc | BnO-PEG5-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. |
T15761 | Lipoamide-PEG3-Mal | Lipoamide-PEG3-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. |
T17518 | Azido-PEG6-azide | Azido-PEG6-azide, a PEG-based PROTAC linker, is used in the synthesis of PROTACs [1]. |
T15539 | Hydroxy-PEG8-Boc | Hydroxy-PEG8-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. |
T16231 | N-Mal-N-bis(PEG2-NHS ester) | N-Mal-N-bis(PEG2-NHS ester) is a polyethylene glycol (PEG)-based linker utilized in the synthesis of proteolysis targeting chimeras (PROTACs)[1]. |
T15835 | m-PEG10-amine | m-PEG10-amine is a 10-unit polyethylene glycol (PEG) linker that is non-cleavable. It serves as an essential component in the synthesis of antibody-drug conjugates (ADCs)[1]. Additionally, m-PEG10-amine functions as a PEG-based linker in the synthesis of PROTACs[1], effectively facilitating their formation. |
T18104 | m-PEG-NHS ester (MW 5000) | m-PEG-NHS ester (MW 5000) serves as a PEG-based PROTAC linker for the synthesis of PROTACs[1]. |
T18440 | N-(Mal-PEG6)-N-bis(PEG7-TCO) | N-(Mal-PEG6)-N-bis(PEG7-TCO) is a polyethylene glycol (PEG)-based PROTAC linker employed for PROTAC synthesis[1]. |
T18419 | N-(m-PEG4)-3,3-Dimethyl-3H-indole-N'-(acid-PEG3)-benzothiazole | N-(m-PEG4)-3,3-Dimethyl-3H-indole-N'-(acid-PEG3)-benzothiazole is a PEG-based PROTAC linker suitable for synthesizing PROTACs[1]. |
T18770 | TCO-PEG3-TCO | TCO-PEG3-TCO 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. |
T16305 | NH-bis-PEG3 | NH-bis-PEG3 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. |
T17756 | DBCO-NH-PEG7-C2-NHS ester | DBCO-NH-PEG7-C2-NHS ester is a polyethylene glycol (PEG) derived linker that possesses a terminal DBCO moiety. It functions as an N-hydroxysuccinimide (NHS) ester, making it suitable for the efficient synthesis of proteolysis-targeting chimeras (PROTACs)[1]. |
T15996 | Mal-PEG5-acid | Mal-PEG5-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. |
T18319 | MC-Val-Cit-PAB-Auristatin E | MC-Val-Cit-PAB-Auristatin E is an antibody-drug conjugate (ADC) linker compound featuring Auristatin E, a potent cytotoxic tubulin modifier, connected through the MC-Val-Cit-PAB linker, exhibiting significant antitumor activity. |
T15085 | Dde Biotin-PEG4-DBCO | Dde Biotin-PEG4-DBCO 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. |
T15896 | m-PEG5-NHS ester | m-PEG5-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. |
T16179 | N-(Azido-PEG2)-N-Boc-PEG3-NHS ester | The PEG-based PROTAC linker, N-(Azido-PEG2)-N-Boc-PEG3-NHS ester, is suitable for the synthesis of PROTACs[1]. |