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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
T17433 Amino-PEG36-CONH-PEG36-acid Amino-PEG36-CONH-PEG36-acid is a polyethylene glycol (PEG)-based linker with amino and carboxylic acid functionalities. It finds utility in the synthesis of proteolysis targeting chimeras (PROTACs)[1].
T16320 NHS-PEG4-(m-PEG4)3-ester NHS-PEG4-(m-PEG4)3-ester is a PEG-based PROTAC linker utilized for synthesizing PROTACs[1].
T15509 Hydroxy-Amino-bis(PEG2-propargyl) Hydroxy-Amino-bis(PEG2-propargyl) is a PEG-linked PROTAC linker employed for synthesizing PROTACs[1].
T15872 m-PEG4-Br m-PEG4-Br is a cleavable ADC linker used in the synthesis of an antibody-drug conjugate (ADC) for Trastuzumab. It is positioned distally from the monomethyl auristatin E (MMAE) payload, resulting in an ADC with modified hydrophilicity, antigen binding, and in vivo characteristics.
T14603 Biotin-PEG5-amine Biotin-PEG5-amine is a PEG-based PROTAC linker labeled with biotin. It is utilized in the synthesis of PROTACs, a class of molecules with the ability to target and degrade specific proteins[1].
T14465 Azido-PEG6-acid Azido-PEG6-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.
T14729 Boc-N-Amido-PEG3-azide Boc-N-Amido-PEG3-azide 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.
T14890 Cbz-NH-PEG5-C2-acid Cbz-NH-PEG5-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.
T17989 Gly-PEG3-endo-BCN Gly-PEG3-endo-BCN 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.
T18553 Pomalidomide-amido-PEG3-C2-NH2 Pomalidomide-amido-PEG3-C2-NH2, known as Cereblon Ligand-Linker Conjugates 22, is a synthesized E3 ligase ligand-linker conjugate designed for use in PROTAC technology. It consists of the Pomalidomide-based cereblon ligand and a 3-unit PEG linker. [1]
T17821 Di(N-succinimidyl)adipate Di(N-succinimidyl)adipate, an alkyl chain-based PROTAC linker, facilitates the synthesis of PROTACs[1].
T18262 Mal-NO2-Ph-PEG12-NHS Mal-NO2-Ph-PEG12-NHS 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.
T17618 Bis-PEG13-PFP ester Bis-PEG13-PFP 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.
T18470 N3-PEG16-Hydrazide N3-PEG16-Hydrazide 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.
T17327 2-(Azido-PEG3-amido)-1,3-bis(NHS ester) 2-(Azido-PEG3-amido)-1,3-bis(NHS ester) is a polyethylene glycol (PEG)-based linker for PROTAC synthesis [1].
T17058 Tetrahydropyranyldiethyleneglycol Tetrahydropyranyldiethyleneglycol is a polyethylene glycol (PEG)-based PROTAC linker utilized in the synthesis of PROTACs[1].
T18381 N-(Azido-PEG3)-N-Boc-PEG3-NHS ester N-(Azido-PEG3)-N-Boc-PEG3-NHS ester is a polyethylene glycol (PEG)-based PROTAC linker, specifically designed for the synthesis of PROTACs[1].
T18206 m-PEG48-OH m-PEG48-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.
T14586 Biotin-PEG2-Mal Biotin-PEG2-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.
T18039 Hydroxy-PEG16-Boc Hydroxy-PEG16-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.
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