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
T14600	Biotin-PEG4-methyltetrazine	Biotin-PEG4-methyltetrazine is a PEG-derived linker utilized for synthesizing PROTACs[1], a type of molecule employed in targeted protein degradation.
T18249	Mal-C6-α-Amanitin	Mal-C6-α-Amanitin is a drug-linker conjugate for ADC with potent antitumor activity by using α-Amanitin (an RNA polymerase II inhibitor), linked via the ADC linker Mal-C6.
T14397	Azide-PEG5-Tos	Azide-PEG5-Tos is a cleavable PEG linker consisting of five units, employed for the synthesis of antibody-drug conjugates (ADCs)[1].
T18036	Hydroxy-PEG12-CH2-Boc	Hydroxy-PEG12-CH2-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.
T17392	Amine-PEG-amine (MW 3400)	Amine-PEG-amine (MW 3400) is a polyethylene glycol (PEG) -based linker used for synthesizing proteolysis-targeting chimeras (PROTACs)[1].
T17138	Tos-PEG6-OH	Tos-PEG6-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.
T18491	NH2-PEG4-Lys(Boc)-NH-(m-PEG24)	NH2-PEG4-Lys(Boc)-NH-(m-PEG24) is a 28-unit polyethylene glycol (PEG) linker containing a cleavable bond, commonly employed in the production of antibody-drug conjugates (ADCs)[1].
T18343	Methyltetrazine-PEG24-amine	Methyltetrazine-PEG24-amine is a PEG-conjugated PROTAC linker utilized for the synthesis of PROTACs[1].
T17827	Diketone-PEG12-DBCO	Diketone-PEG12-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.
T16624	Propargyl-PEG4-CH2CH2-Boc	Propargyl-PEG4-CH2CH2-Boc is a PEG- and Alkyl/ether-based non-cleavable ADC linker. Propargyl-PEG5-Boc can be used to synthesize ADC inhibitors of Galectin-3[1].
T15972	Mal-NH2 TFA	Mal-NH2 TFA is a alkyl chain-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.
T17635	Bis-Tos-PEG6	Bis-Tos-PEG6 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.
T14246	Amino-PEG5-CH2COOH	Amino-PEG5-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.
T15149	DNP-NH-PEG4-C2-Boc	DNP-NH-PEG4-C2-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.
T14398	Azide-PEG6-Tos	Azide-PEG6-Tos 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.
T15875	m-PEG4-CH2-acid	m-PEG4-CH2-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.
T18306	MC-Alkyl-Hydrazine Modified MMAF	MC-Alkyl-Hydrazine Modified MMAF is a potent antitumor drug-linker conjugate for ADC, incorporating Modified MMAF, a tubulin inhibitor, through a noncleavable MC-Alkyl-Hydrazine linkage[1].
T14803	Bromo-PEG4-bromide	Bromo-PEG4-bromide 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.
T14530	Benzenedimethanamine-diethylamine	Benzenedimethanamine-diethylamine is a derivatized linker compound derived from an alkyl chain. It serves as a valuable component in the synthesis of PROTACs, a class of compounds used for targeted protein degradation[1].
T18864	UAA crosslinker 1	UAA crosslinker 1 hydrochloride is an Amber codon-activating agent utilized for the incorporation of non-canonical amino acids (ncAAs) into proteins. This incorporation is achieved in vivo by leveraging the promiscuous activity of specific wildtype and engineered aminoacyl-tRNA synthetases[1].

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PROTAC Linker