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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
T17634 Bis-propargyl-PEG13 Bis-propargyl-PEG13 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.
T15870 m-PEG4-azide m-PEG4-azide, also referred to as 13-Azido-2,5,8,11-tetraoxatridecane, functions as a PEG-based PROTAC linker suitable for PROTACs synthesis[1].
T14602 Biotin-PEG4-OH Biotin-PEG4-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.
T15491 HO-PEG17-OH HO-PEG17-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.
T18455 N,N'-bis-(azide-PEG3)-Cy5 NN'-bis-(azide-PEG3)-Cy5 is a polyethylene glycol (PEG) derived linker designed for the synthesis of proteolysis-targeting chimeras (PROTACs)[1].
T16647 Propargyl-PEG8-NHS ester Propargyl-PEG8-NHS ester, a cleavable ADC linker, is utilized in the synthesis of antibody-drug conjugates (ADCs) [1].
T17897 cIAP1 Ligand-Linker Conjugates 13 cIAP1 Ligand-Linker Conjugates 13, containing an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker, are utilized in the development of SNIPERs[1].
T16065 Methyltetrazine-propylamine Methyltetrazine-propylamine is an alkyl chain-based PROTAC linker utilized for the synthesis of PROTACs[1].
T17395 Amine-PEG-CH2COOH (MW 5000) Amine-PEG-CH2COOH (MW 5000) is a polyethylene glycol (PEG) derivative employed as a linker in the synthesis of proteolysis targeting chimeras (PROTACs)[1].
T14233 Amino-PEG3-C2-Amine Amino-PEG3-C2-Amine, a PEG-based linker with three units, is utilized in PROTAC synthesis.
T17388 AM-Imidazole-PA-Boc AM-Imidazole-PA-Boc is an alkyl chain-derived PROTAC linker utilized for the synthesis of PROTAC IRAK4 degrader-1[1].
T14253 Amino-PEG9-acid Amino-PEG9-acid is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
T14478 Azido-PEG8-CH2COO-PFP Azido-PEG8-CH2COO-PFP 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.
T18534 PEG4-aminooxy-MMAF PEG4-aminooxy-MMAF is a drug-linker conjugate designed for antibody-drug conjugates (ADC) that exhibits potent antitumor activity. It incorporates MMAF, a powerful antitubulin agent, connected through a non-cleavable PEG4 linker[1].
T14273 Aminooxy-PEG4-C2-Boc Aminooxy-PEG4-C2-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.
T15309 Fmoc-N-methyl-PEG3-CH2CH2COOH Fmoc-N-methyl-PEG3-CH2CH2COOH is a cleavable ADC linker utilized in the synthesis of antibody-drug conjugates (ADCs) [1].
T17620 Bis-PEG15-acid Bis-PEG15-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.
T17448 AmPEG6C2-Aur0131 AmPEG6C2-Aur0131 is a drug-linker conjugate designed for anti-CXCR4 ADC applications, showcasing potent antitumor activity. It incorporates Aur0131, an auristatin-based microtubule inhibitor, connected through the non-cleavable AmPEG6C2 linker.
T18073 Lipoamido-PEG12-acid Lipoamido-PEG12-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.
T17805 DBCO-PEG6-amine DBCO-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.
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