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
T17899	cIAP1 Ligand-Linker Conjugates 9	cIAP1 Ligand-Linker Conjugates 9 feature an IAP ligand specifically targeting the E3 ubiquitin ligase, along with a PROTAC linker. It is valuable tools for developing SNIPERs[1].
T16607	Propargyl-PEG3-Boc	Propargyl-PEG3-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.
T18653	S-(1-Hydroxy-2-methylpropan-2-yl) methanesulfonothioate	S-(1-Hydroxy-2-methylpropan-2-yl) methanesulfonothioate, an ADC linker, is a glutathione cleavable compound used for the attachment of monoclonal antibodies (mAb) in antibody-drug conjugates (ADCs). It specifically refers to the Alkyl-Chain composition of the linker portion of these molecules [1].
T14662	Bis-propargyl-PEG9	Bis-propargyl-PEG9 is a PEG-based PROTAC linker employed in the synthesis of PROTACs. It is specifically utilized to synthesize the bivalent ligands of estrogen receptor[1].
T18092	m-PEG-mal (MW 10000)	m-PEG-mal (MW 10000) 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.
T17776	DBCO-PEG1-acid	DBCO-PEG1-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.
T15938	m-PEG8-thiol	m-PEG8-thiol 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.
T18827	Thalidomide-O-PEG4-amine	Thalidomide-O-PEG4-amine is a PEG-based PROTAC linker used in the synthesis of PROTACs [1].
T15086	Dde Biotin-PEG4-Picolyl azide	Dde Biotin-PEG4-Picolyl azide is a PEG-based PROTAC linker used for synthesizing PROTACs[1].
T18556	Pomalidomide-PEG4-azide	Pomalidomide-PEG4-azide is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
T17815	DBCO-Val-Cit-PABC-OH	DBCO-Val-Cit-PABC-OH is a cleavable linker employed in the synthesis of antibody-drug conjugates (ADCs) [1].
T14519	BDP FL-PEG5-azide	BDP FL-PEG5-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.
T15521	Hydroxy-PEG2-CH2COOH	Hydroxy-PEG2-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.
T14427	Azido-PEG3-C3-OH	Azido-PEG3-C3-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.
T17564	Biotin-PEG2-C1-aldehyde	Biotin-PEG2-C1-aldehyde is a polyethylene glycol (PEG)-based linker utilized in synthesizing proteolysis targeting chimeras (PROTACs) [1].
T15314	Fmoc-NH-PEG1-CH2COOH	Fmoc-NH-PEG1-CH2COOH is a cleavable ADC linker utilized in the synthesis of antibody-drug conjugates (ADCs)[1].
T17932	endo-BCN-PEG12-acid	endo-BCN-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.
T17721	Cbz-NH-PEG24-C2-acid	Cbz-NH-PEG24-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.
T17335	4-Methyl-4-(pyridin-2-yldisulfanyl)pentanoic acid	4-Methyl-4-(pyridin-2-yldisulfanyl)pentanoic acid is a cleavable linker compound employed in the synthesis of antibody-drug conjugates (ADCs)[1].
T17546	Biotin-C1-PEG3-C3-amine TFA	Biotin-C1-PEG3-C3-amine (TFA) is a polyethylene glycol (PEG) based linker that serves as a crucial component in the synthesis of proteolysis targeting chimeras (PROTACs)[1].

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PROTAC Linker