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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
T18165 m-PEG24-acid m-PEG24-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.
T14619 Bis-aminooxy-PEG3 Bis-aminooxy-PEG3 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.
T17754 DBCO-NH-Boc DBCO-NH-Boc is a alkyl/ether-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.
T17317 1,1,1-Trifluoroethyl-PEG2-propargyl 1,1,1-Trifluoroethyl-PEG2-propargyl is a polyethylene glycol (PEG) derivative designed specifically to serve as a PROTAC linker in the synthesis of PROTACs[1].
T16204 N-Boc-N-bis(PEG2-OH) N-Boc-N-bis(PEG2-OH) is a cleavable ADC linker utilized in the synthesis of antibody-drug conjugates (ADCs)[1].
T17990 H2N-PEG12-Hydrazide H2N-PEG12-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.
T16008 Maleimido-tri(ethylene glycol)-propionic acid Maleimido-tri(ethylene glycol)-propionic acid is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Maleimido-tri(ethylene glycol)-propionic acid is used for the preparation of neolymphostin-based ADC precursors for site-spec
T17674 Boc-NH-PEG23-NH2 Boc-NH-PEG23-NH2 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.
T18227 m-PEG9-Hydrazide m-PEG9-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.
T17676 Boc-NH-PEG3-C2-triazole-DBCO-PEG4-VC-PAB-DMEA Boc-NH-PEG3-C2-triazole-DBCO-PEG4-VC-PAB-DMEA is a double-cleavable PEG linker (3-unit and 4-unit) designed for antibody-drug conjugation (ADC).
T14618 Bis-aminooxy-PEG2 Bis-aminooxy-PEG2 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.
T18289 Mal-PEG4-VA-PBD Mal-PEG4-VA-PBD is a drug-linker conjugate for Antibody-Drug Conjugates (ADCs), comprising the antitumor antibiotic Pyrrolobenzodiazepine (PBD), connected through Mal-PEG4-VA.
T15848 m-PEG2-Tos m-PEG2-Tos is an uncleavable ADC linker utilized in the synthesis of antibody-drug conjugates (ADCs).
T17980 Fmoc-Phe-Lys(Trt)-PAB-PNP Fmoc-Phe-Lys(Trt)-PAB-PNP is a cleavable linker for antibody-drug conjugate (ADC) synthesis, specifically designed for use in ADC synthesis.
T17013 TCO-C3-PEG3-C3-amine TCO-C3-PEG3-C3-amine 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.
T18248 Mal-C2-NHS ester Mal-C2-NHS ester is a noncleavable linker compound commonly employed for the synthesis of antibody-drug conjugates (ADCs)[1].
T18450 N-methyl-N'-methyl-O-(m-PEG4)-O'-(propargyl-PEG4)-Cy3 N-methyl-N'-methyl-O-(m-PEG4)-O'-(propargyl-PEG4)-Cy3 is a polyethylene glycol (PEG)-based linker used for the synthesis of proteolysis targeting chimeras (PROTACs) [1].
T17153 Tr-PEG6-OH Tr-PEG6-OH is a 6-unit polyethylene glycol (PEG) linker, which is non-cleavable and extensively employed in the synthesis of antibody-drug conjugates (ADCs).
T15068 DBCO-PEG4-amine DBCO-PEG4-amine is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). DBCO-PEG4-amine can be used in the synthesis of FPM-PEG4-DBCO (a homobifunctional azide-to-azide cross-linker)[1].
T14752 Boc-NH-PEG6-CH2CH2COOH Boc-NH-PEG6-CH2CH2COOH is a cleavable ADC linker employed in antibody-drug conjugates (ADC).
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