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
T16051	Methylamino-PEG3-azide	Methylamino-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.
T13993	1-Isothiocyanato-PEG3-azide	1-Isothiocyanato-PEG3-azide is a PEG-based PROTAC linker utilized for PROTAC synthesis[1].
T17882	Pomalidomide-PEG3-C2-NH2 (TFA)	Pomalidomide-PEG3-C2-NH2 TFA is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and 3-unit PEG linker used in PROTAC technology.
T15920	m-PEG7-Amine	m-PEG7-Amine is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
T18857	Tri(Amino-PEG3-amide)-amine	Tri(Amino-PEG3-amide)-amine is a polyethylene glycol (PEG)-derived linker employed for the synthesis of proteolysis-targeting chimeric molecules (PROTACs)[1].
T17614	Bis-PEG11-NHS ester	Bis-PEG11-NHS 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.
T16185	N-(Azido-PEG3)-N-bis(PEG1-t-butyl ester)	N-(Azido-PEG3)-N-bis(PEG1-t-butyl ester) is a polyethylene glycol (PEG)-based PROTAC linker utilized for the synthesis of PROTACs[1].
T18619	Bis-PEG1-C-PEG1-CH2COOH	Bis-PEG1-C-PEG1-CH2COOH (PROTAC Linker 26) is a PEG-based linker suitable for the synthesis of PROTACs, compound complexes that selectively degrade target proteins[1].
T16600	Propargyl-PEG2-Ms	Propargyl-PEG2-Ms 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.
T16633	Propargyl-PEG4-tetra-Ac-beta-D-glucose	Propargyl-PEG4-tetra-Ac-beta-D-glucose, a PEG-based PROTAC linker, facilitates the synthesis of PROTACs[1].
T17775	DBCO-NHS ester 3	DBCO-NHS ester 3 (Compound 12) is a cleavable linker utilized in the synthesis of antibody-drug conjugate (ADC). It is a derivative of Dibenzylcyclooctyne (DBCO) resulting from the activation of N-hydroxysuccinimide by the carboxylic acid moiety of both methyl-oxanorbornadiene (MeOND) and dibenzoazacyclooctyne (DIBAC)[1][2].
T18727	Sulfo-SIAB	Sulfo-SIAB, a noncleavable monovalent bilinker, is designed for specific applications where a stable, non-reducible linkage is required.
T18345	Methyltetrazine-PEG24-NH-Boc	Methyltetrazine-PEG24-NH-Boc is a PEG-derived linker for PROTAC synthesis[1].
T17880	E3 ligase Ligand 9	E3 ligase Ligand 9 is a compound that serves as a ligand for E3 ubiquitin ligase. It can be linked to the protein ligand through a linker, forming PROTACs or SNIPERs. These PROTACs are known to induce the degradation of cancer-promoting proteins through ubiquitination-mediated mechanisms[1].
T18292	Mal-PEG4-VC-PAB-DMEA-PNU-159682	Mal-PEG4-VC-PAB-DMEA-PNU-159682 is a drug-linker conjugate designed for antibody-drug conjugate (ADC) therapy. It combines the ADC linker, Mal-PEG4-VC-PAB, with the potent ADC cytotoxin, DMEA-PNU-159682. The cytotoxin, DMEA-PNU-159682, is derived from metabolites of nemorubicin (MMDX) found in liver microsomes, as well as the ADC cytotoxin PNU-159682[1].
T13994	1-Isothiocyanato-PEG4-alcohol	1-Isothiocyanato-PEG4-alcohol is a polyethylene glycol (PEG)-derived linker compound suitable for the incorporation into Proteolysis Targeting Chimeras (PROTACs)[1].
T14728	Boc-N-amido-PEG3-acid	Boc-N-amido-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.
T16214	N-(Boc-PEG3)-N-bis(PEG3-azide)	N-(Boc-PEG3)-N-bis(PEG3-azide) is a polyethylene glycol (PEG)-based linker, specifically designed for the synthesis of proteolysis targeting chimeras (PROTACs) [1].
T18240	Mal-amido-PEG2-Val-Cit-PAB-OH	Mal-amido-PEG2-Val-Cit-PAB-OH is a bi-functional polyethylene glycol (PEG) linker, comprised of two PEG units, that can be cleaved. It is specifically designed for the synthesis of antibody-drug conjugates (ADCs)[1].
T15987	Mal-PEG3-NHS ester	Mal-PEG3-NHS ester, a noncleavable ADC linker, possesses a Maleimide group. It serves as a crucial component in the synthesis of antibody-drug conjugates[1].

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PROTAC Linker