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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
T17127 Tos-PEG3-C2-methyl ester Tos-PEG3-C2-methyl ester is a polyethylene glycol (PEG)-based linker utilized for the synthesis of PROteolysis TArgeting Chimeras (PROTACs)[1].
T15916 m-PEG6-O-CH2COOH m-PEG6-O-CH2COOH 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.
T17975 Fmoc-NH-pentanoic acid-NHS-SO3Na Fmoc-NH-pentanoic acid-NHS-SO3Na is a PROTAC linker molecule derived from an alkyl chain. It possesses the ability to facilitate the synthesis of PROTACs[1].
T18858 Tri(Amino-PEG4-amide)-amine Tri(Amino-PEG4-amide)-amine is a polyethylene glycol (PEG)-based linker compound utilized for the synthesis of proteolysis-targeting chimeras (PROTACs)[1].
T18301 Mal-Phe-C4-Val-Cit-PAB Mal-Phe-C4-Val-Cit-PAB is a cleavable antibody-drug conjugate (ADC) linker featuring a Maleimide functional group. It is employed in the synthesis of ADCs.
T17589 Biotin-PEG6-amine Biotin-PEG6-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.
T18129 m-PEG11-OH m-PEG11-OH 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.
T18425 N-(m-PEG4)-N'-(azide-PEG4)-Cy7 N-(m-PEG4)-N'-(azide-PEG4)-Cy7 is a polyethylene glycol (PEG)-based linker utilized for the synthesis of proteolysis targeting chimeras (PROTACs)[1].
T14014 2-(Biotin-amido)-1,3-bis-(C1-PEG1-acid) 2-(Biotin-amido)-13-bis(carboxylethoxy)propane is a polyethylene glycol (PEG)-based PROteolysis TArgeting Chimera (PROTAC) linker utilized in the synthesis of PROTACs[1].
T18353 Methyltetrazine-PEG5-methyltetrazine Methyltetrazine-PEG5-methyltetrazine is a PEG-based PROTAC linker utilized for the synthesis of PROTACs[1].
T14286 ANB-NOS ANB-NOS is a alkyl/ether-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.
T17981 Fmoc-Phe-Lys(Boc)-PAB-PNP Fmoc-Phe-Lys(Boc)-PAB-PNP is a cleavable antibody-drug conjugate (ADC) linker employed in the synthesis of ADCs.
T14702 BnO-PEG6-OH BnO-PEG6-OH is a non-cleavable, 6-unit PEG linker used in the synthesis of antibody-drug conjugates (ADCs).
T16186 N-(Azido-PEG3)-N-bis(PEG3-acid) N-(Azido-PEG3)-N-bis(PEG3-acid) is a polyethylene glycol (PEG)-based linker that incorporates an azido group and two PEG3-acid moieties. This compound is widely applicable in the synthesis of proteolysis targeting chimeras (PROTACs), which are molecules with the ability to selectively degrade target proteins[1].
T18148 m-PEG14-amine m-PEG14-amine is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
T14041 4-Maleimidobutyric acid 4-Maleimidobutyric acid is an alkyl chain-derived PROTAC linker that enables the synthesis of PROTACs[1].
T16630 Propargyl-PEG4-O-C1-NHS ester Propargyl-PEG4-O-C1-NHS ester, also known as compound 8, is a polyethylene glycol (PEG)-based linker that serves as a reactive functional group for the synthesis of proteolysis targeting chimeras (PROTACs).
T15884 m-PEG4-propargyl m-PEG4-propargyl 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.
T16599 Propargyl-PEG3-NHS ester Propargyl-PEG3-NHS ester, a cleavable ADC linker, is utilized in the synthesis of antibody-drug conjugates (ADCs)[1].
T18293 Mal-PEG4-VC-PAB-DMEA-Seco-Duocarmycin SA Mal-PEG4-VC-PAB-DMEA-Seco-Duocarmycin SA is an antibody-drug conjugate linker that incorporates the antitumor antibiotic Duocarmycin SA, connected through the Mal-PEG4-VC-PAB-DMEA-Seco linker, for targeted cancer therapy.
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