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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
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].
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