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
T17664	Boc-NH-PEG11-CH2CH2N3	Boc-NH-PEG11-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.
T15515	Hydroxy-PEG2-acid	Hydroxy-PEG2-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.
T18590	Propargyl-PEG7-methane	Propargyl-PEG7-methane 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.
T18740	t-Boc-Aminooxy-PEG12-NHS ester	t-Boc-Aminooxy-PEG12-NHS ester is a polyethylene glycol (PEG) derived PROTAC linker, specifically designed for the synthesis of PROTACs[1].
T14743	Boc-NH-PEG3-sulfonic acid	Boc-NH-PEG3-sulfonic acid is a polyethylene glycol (PEG) derived linker used for the synthesis of proteolysis-targeting chimeras (PROTACs)[1].
T18493	NH2-PEG5-C6-Cl	NH2-PEG5-C6-Cl (K-7) is a PROTAC linker characterized by its PEG composition. It can be utilized in the synthesis of various PROTACs, facilitating the degradation of intracellular molecules via autophagy[1].
T17340	5-endo-BCN-pentanoic acid	5-endo-BCN-pentanoic acid, an alkyl chain-based PROTAC linker, facilitates the synthesis of PROTACs[1].
T16211	N-Boc-PEG2-bromide	N-Boc-PEG2-bromide, a cleavable ADC linker, is utilized in the synthesis of antibody-drug conjugates (ADCs)[1].
T14655	Bis-propargyl-PEG2	Bis-propargyl-PEG2, a PEG-based PROTAC linker, facilitates the synthesis of PROTACs and demethylvancomycin dimers[1][2].
T14231	Amino-PEG2-NH-Boc	Amino-PEG2-NH-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.
T17809	DBCO-PEG9-DBCO	DBCO-PEG9-DBCO 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.
T14434	Azido-PEG3-SS-PEG3-azide	Azido-PEG3-SS-PEG3-azide is a polyethylene glycol (PEG) based linker commonly employed in the synthesis of proteolysis targeting chimeras (PROTACs)[1].
T18178	m-PEG3-Hydrazide	m-PEG3-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.
T18337	Methyltetrazine-amido-PEG5-alkyne	Methyltetrazine-amido-PEG5-alkyne is a polyethylene glycol (PEG) derivative commonly employed as a linker for proteolysis targeting chimeras (PROTACs) synthesis [1].
T17930	EC1167	EC1169 is a targeted tubulysin conjugate that utilizes EC1167 as its linker. This compound shows promise in the treatment of recurrent metastatic, castration-resistant prostate cancer (MCRPC)[1].
T18154	m-PEG16-Mal	m-PEG16-Mal 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.
T15980	Mal-PEG2-NH-Boc	Mal-PEG2-NH-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.
T14236	Amino-PEG3-CH2COOH	Amino-PEG3-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.
T14109	Acid-PEG5-mono-methyl ester	Acid-PEG5-mono-methyl ester, a PEG-based PROTAC linker, enables the synthesis of PROTACs[1].
T18543	Phthalimide-PEG4-MPDM-OH	Phthalimide-PEG4-MPDM-OH, a PROTAC linker with a PEGs composition, has applications in the synthesis of various PROTACs. These PROTACs consist of a linker connecting two distinct ligands: one binds to an E3 ubiquitin ligase, while the other binds to the target protein. By leveraging the intracellular ubiquitin-proteasome system, PROTACs selectively induce the degradation of target proteins [1].

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PROTAC Linker