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
T18304	Mal-VC-PAB-ABAEP-Azonafide	Mal-VC-PAB-ABAEP-Azonafide, an ADC (antibody-drug conjugate) linker-drug conjugate, demonstrates potent antitumor activity. It incorporates Azonafide, a cytotoxin, connected through the ADC linker Mal-VC-PAB[1].
T18576	Propargyl-PEG24-amine	Propargyl-PEG24-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.
T18862	Triethylene glycol monobenzyl ether	Triethylene glycol monobenzyl ether, a PEG-derived PROTAC linker, facilitates the synthesis of PROTACs[1].
T17455	AZD-CO-C2-Ph-amido-Ph-azide	AZD-CO-C2-Ph-amido-Ph-azide is an alkyl chain-derived PROTAC linker suitable for PROTACs synthesis[1].
T16146	Ms-PEG12-m	Ms-PEG12-m 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.
T18754	TCO-PEG1-Val-Cit-PABC-OH	TCO-PEG1-Val-Cit-PABC-OH, a cleavable 1-unit PEG ADC linker, is employed in the synthesis of antibody-drug conjugates (ADCs)[1].
T18367	Ms-PEG12-Boc	Ms-PEG12-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.
T18043	Hydroxy-PEG4-C2-methyl ester	Hydroxy-PEG4-C2-methyl ester is a PEG-based PROTAC linker employed in PROTAC synthesis[1].
T14816	Bromoacetamido-C2-PEG2-NH-Boc	Bromoacetamido-C2-PEG2-NH-Boc is a polyethylene glycol (PEG)-based linker with a bromoacetamido functional group and a tert-butoxycarbonyl (Boc) protecting group. It serves as an integral component in the synthesis of proteolysis-targeting chimeras (PROTACs), which are innovative compounds used for targeted protein degradation[1].
T17617	Bis-PEG13-NHS ester	Bis-PEG13-NHS ester, a cleavable ADC linker, is utilized in the synthesis of antibody-drug conjugates (ADCs) [1].
T18762	TCO-PEG3-acid	TCO-PEG3-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.
T18452	N-methyl-N'-(propargyl-PEG4)-Cy5	N-methyl-N'-(propargyl-PEG4)-Cy5 (chloride) is a PEG-based PROTAC linker suitable for PROTAC synthesis[1].
T14708	Boc-aminooxy-PEG1-propargyl	Boc-aminooxy-PEG1-propargyl is a polyethylene glycol (PEG)-based linker commonly employed in the synthesis of proteolysis targeting chimeras (PROTACs)[1].
T18233	Mal-amido-PEG1-C2-NHS ester	Mal-amido-PEG1-C2-NHS ester is a noncleavable antibody-drug conjugate (ADC) linker that incorporates a maleimide functional group and an N-hydroxysuccinimide (NHS) ester. The NHS ester offers a means to specifically modify primary amines (-NH2) present in proteins, amine-modified oligonucleotides, and other amine-containing molecules[1][2].
T14163	Ald-Ph-amido-C2-PEG3-NH-Boc	Ald-Ph-amido-C2-PEG3-NH-Boc is a polyethylene glycol (PEG)-based bifunctional linker utilized for the synthesis of Proteolysis Targeting Chimeras (PROTACs)[1].
T17088	THP-SS-PEG1-Boc	THP-SS-PEG1-Boc is a cleavable ADC linker comprising a one-unit PEG, commonly employed in the synthesis of antibody-drug conjugates (ADCs)[1].
T15838	m-PEG11-Amine	m-PEG11-Amino is a cleavable ADC linker utilized in the synthesis of antibody-drug conjugates (ADCs)[1].
T16983	TAMRA-PEG4-acid	TAMRA-PEG4-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.
T18313	Mc-O-Si(di-iso)-Cl	Mc-O-Si(di-iso)-Cl is a cleavable ADC linker, commonly employed in the synthesis of antibody-drug conjugates (ADCs) like Gemcitabine-O-Si(di-iso)-O-Mc [1].
T16213	N-(Boc-PEG3)-N-bis(PEG2-alcohol)	N-(Boc-PEG3)-N-bis(PEG2-alcohol) is a polyethylene glycol (PEG) based linker commonly employed in the synthesis of proteolysis-targeting chimeras (PROTACs)[1].

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PROTAC Linker