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
T18722	MAC glucuronide α-hydroxy lactone-linked SN-38	MAC glucuronide α-hydroxy lactone-linked SN-38 (Topoisomerase I inhibitor) is a stabilized lactone MAC glucuronide α-hydroxy lactone-linked SN-38 drug linker. MAC glucuronide α-hydroxy lactone-linked SN-38 is cytotoxic across L540cy cells and Ramos cells
T14464	Azido-PEG5-succinimidyl carbonate	Azido-PEG5-succinimidyl carbonate is a polyethylene glycol (PEG) derivative with a linked succinimidyl carbonate and azido group. It serves as a PEG-based PROTAC linker for the synthesis of PROTACs[1].
T14259	Aminooxy-PEG1-azide	Aminooxy-PEG1-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.
T18544	Phthalimide-PEG4-PDM-OTBS	Phthalimide-PEG4-PDM-OTBS is a PROTAC linker comprised of polyethylene glycols (PEGs). This compound is utilized in the synthesis of a range of PROTACs, which consists of two distinct ligands connected by a linker. One ligand binds to an E3 ubiquitin ligase, while the other ligand binds to the target protein. By leveraging the intracellular ubiquitin-proteasome system, PROTACs selectively degrade target proteins[1].
T17639	Boc-amino-PEG3-SS-acid	Boc-amino-PEG3-SS-acid is a three-unit polyethylene glycol (PEG) linker with cleavable properties. It is commonly employed in the synthesis of antibody-drug conjugates (ADCs)[1].
T15527	Hydroxy-PEG3-SS-PEG3-alcohol	Hydroxy-PEG3-SS-PEG3-alcohol is a 6 unit polyethylene glycol (PEG) linker that can be cleaved. It is commonly employed in the synthesis of antibody-drug conjugates (ADCs) [1].
T17672	Boc-NH-PEG20-CH2CH2COOH	Boc-NH-PEG20-CH2CH2COOH, a PEG-based PROTAC linker, facilitates the synthesis of PROTACs[1].
T18377	N-(Azide-PEG3)-N'-(PEG4-acid)-Cy5	N-(Azide-PEG3)-N'-(PEG4-acid)-Cy5 is a PEG-based PROTAC linker employed for PROTACs (proteolysis-targeting chimeras) synthesis[1].
T18627	Tos-PEG3-O-C1-CH3COO	Tos-PEG3-O-C1-CH3COO (PROTAC Linker 6) is a PEG-based linker compound that finds utility in the synthesis of PROTACs[1].
T18111	m-PEG-thiol (MW 5000)	m-PEG-thiol (MW 5000) 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.
T18130	m-PEG11-SH	m-PEG11-SH 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.
T15881	m-PEG4-NHS ester	m-PEG4-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.
T14432	Azido-PEG3-O-NHS ester	Azido-PEG3-O-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.
T14247	Amino-PEG6-alcohol	Amino-PEG6-OH is a non-cleavable 6 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
T18600	VH032 thiol	VH032 thiol (VHL ligand 6) is a VHL ligand that interacts with pan-BET inhibitor JQ1 through a linker to create a PROTAC[1] compound.
T18861	Triethylene glycol bis(p-toluenesulfonate)	Triethylene glycol bis(p-toluenesulfonate) is a polyethylene glycol (PEG) derived linker compound, utilized for the synthesis of PROteolysis TArgeting Chimeras (PROTACs)[1].
T17435	Amino-PEG4-Val-Cit-PAB-MMAE	Amino-PEG4-Val-Cit-PAB-MMAE is a cleavable tetraethylene glycol (4 unit PEG) antibody-drug conjugate (ADC) linker employed in the synthesis of ADCs[1].
T17759	DBCO-NHCO-PEG12-biotin	DBCO-NHCO-PEG12-biotin 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.
T17535	BCN-PEG4-hydrazide	BCN-PEG4-hydrazide 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.
T18024	HS-PEG3-CH2CH2NH2	HS-PEG3-CH2CH2NH2 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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PROTAC Linker