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
T18849	Tos-PEG13-Boc	Tos-PEG13-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.
T17881	(S,R,S)-AHPC-C10-NH2	(S,R,S)-AHPC-C10-NH2 (VH032-C10-NH2) 包含基于 (S,R,S)-AHPC 的VHL 配体和 1 个 linker，是一种合成的 E3 连接酶配体-linker 偶联物 (E3 ligase ligand-linker conjugate)。用于 BET 的靶向 PROTAC 的合成。
T14869	Carboxy-PEG4-sulfonic acid	Carboxy-PEG4-sulfonic acid is a PEG-based linker commonly employed in PROTAC synthesis [1].
T18103	m-PEG-NHS ester (MW 20000)	rm-PEG-NHS ester (MW 20000) is a PEG-based PROTAC linker utilized for the synthesis of PROTACs[1].
T14164	Ald-Ph-amido-PEG2-C2-Boc	Ald-Ph-amido-PEG2-C2-Boc is a polyethylene glycol (PEG)-based linker utilized for the synthesis of proteolysis targeting chimeras (PROTACs)[1].
T16183	N-(Azido-PEG2)-N-Fluorescein-PEG3-acid	N-(Azido-PEG2)-N-Fluorescein-PEG3-acid is a polyethylene glycol (PEG)-derived PROTAC linker specifically designed for the synthesis of PROTACs[1].
T18703	SPDB-sulfo	SPDB-sulfo, a glutathione-cleavable linker, is utilized in the development of antibody-drug conjugates (ADCs) [1].
T17333	4-(6-Methyl-1,2,4,5-tetrazin-3-yl)phenol	4-(6-Methyl-1,2,4,5-tetrazin-3-yl)phenol is an alkyl chain-derived PROTAC linker employed for the synthesis of PROTACs[1].
T14243	Amino-PEG5-amine	Amino-PEG5-amine, a PEG-based linker containing 5 units, is utilized in PROTAC synthesis.
T18784	TCO-PEG9-maleimide	TCO-PEG9-maleimide 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.
T18094	m-PEG-mal (MW 20000)	m-PEG-mal (MW 20000) 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.
T17703	Bromoacetamido-PEG9-ethylcarbamoyl-C4-Boc	Bromoacetamido-PEG9-ethylcarbamoyl-C4-Boc is a polyethylene glycol (PEG)-based proteolysis targeting chimera (PROTAC) linker, used for synthesizing PROTACs[1].
T16252	N-(t-Boc-Aminooxy-PEG2)-N-bis(PEG3-propargyl)	N-(t-Boc-Aminooxy-PEG2)-N-bis(PEG3-propargyl) is a polyethylene glycol (PEG) derivative specifically designed as a linker for PROTAC synthesis [1].
T15499	HOOCCH2O-PEG4-CH2COOH	HOOCCH2O-PEG4-CH2COOH (compound 5), is a symmetric polyethylene glycol (PEG) linker. It is primarily utilized in the synthesis of the initial Homo-PROTAC[1] compound.
T18724	Sulfo-DMAC-SPP	Sulfo-DMAC-SPP is an ADC linker employed for the synthesis of antibody-drug conjugates (ADCs) [1].
T18025	HS-PEG5-CH2CH2N3	HS-PEG5-CH2CH2N3 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.
T18480	NH-bis(C1-PEG1-Boc)	NH-bis(C1-PEG1-Boc) is an alkyl/ether-based PROTAC linker utilized for PROTAC synthesis[1].
T14262	Aminooxy-PEG2-azide	Aminooxy-PEG2-azide is a PEG-based PROTAC linker utilized for the synthesis of PROTACs[1], as well as a non-cleavable 2-unit PEG ADC linker employed in the synthesis of antibody-drug conjugates (ADCs)[2].
T17447	Aminoxyacetamide-PEG3-azide	Aminoxyacetamide-PEG3-azide is a non-cleavable 3-unit polyethylene glycol linker employed for antibody-drug conjugate (ADC) synthesis[1].
T16180	N-(Azido-PEG2)-N-Boc-PEG4-acid	N-(Azido-PEG2)-N-Boc-PEG4-acid is a polyethylene glycol (PEG)-based linker specifically designed for the synthesis of PROteolysis TArgeting Chimeras (PROTACs)[1].

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PROTAC Linker