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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
T18786 TCO-SS-amine TCO-SS-amine is a cleavable linker vital in ADC synthesis. TCO-SS-amine joins cytotoxic drugs to antibodies, enabling precise delivery to cells or proteins. The cleavable nature ensures controlled drug release, optimizing ADC effectiveness.
T17331 (2-pyridyldithio)-PEG4 acid (2-Pyridyldithio)-PEG4 acid is a four-unit cleavable polyethylene glycol (PEG) linker specifically designed for the synthesis of antibody-drug conjugates (ADCs)[1]. It serves as a crucial component in the conjugation of antibodies and drugs, enabling targeted drug delivery and enhanced therapeutic efficacy. This linker possesses a (2-pyridyldithio) group at one end, facilitating the attachment of the linker to the specific site on the antibody molecule. The PEG4 chain provides the necessary flexibility and biocompatibility for optimal drug release while maintaining stability throughout the circulation in the body. Ultimately, (2-Pyridyldithio)-PEG4 acid is instrumental in the development and advancement of ADCs, a promising approach in cancer therapy.
T14399 Azide-PEG7-Tos Azide-PEG7-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.
T15855 m-PEG4-CH2-alcohol m-PEG4-CH2-alcohol 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.
T18498 NHPI-PEG3-C2-NHS ester NHPI-PEG3-C2-NHS ester is a three-unit PEG linker compound, noncleavable in nature, specifically employed in the synthesis of antibody-drug conjugates (ADCs).
T17671 Boc-NH-PEG15-NH2 Boc-NH-PEG15-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.
T17513 Azido-PEG4-amido-PEG4-Boc Azido-PEG4-amido-PEG4-Boc is a polyethylene glycol (PEG)-based linker for PROTAC synthesis[1].
T16609 Propargyl-PEG3-CH2COOH Propargyl-PEG3-CH2COOH is a PEG-based PROTAC linker utilized in PROTAC synthesis[1].
T18517 PC Azido-PEG11-NHS carbonate ester PC Azido-PEG11-NHS carbonate ester is a PEG-based PROTAC linker utilized in PROTAC synthesis[1].
T14480 Azido-PEG8-PFP ester Azido-PEG8-PFP 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.
T18433 N-(m-PEG4)-N'-(PEG2-acid)-Cy5 N-(m-PEG4)-N'-(PEG2-acid)-Cy5 is a polyethylene glycol (PEG)-derived linker compound employed in the synthesis of Proteolysis Targeting Chimeras (PROTACs)[1].
T15981 Mal-PEG2-NH2 Mal-PEG2-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.
T18446 N-Methyl-N'-(hydroxy-PEG2)-Cy5 N-Methyl-N'-(hydroxy-PEG2)-Cy5 is a PEG-based linker utilized for the synthesis of PROTACs. It serves as a chemical compound with the ability to facilitate the formation of PROTACs[1].
T17825 Diketone-PEG11-PFP ester Diketone-PEG11-PFP ester serves as a PEG-based PROTAC linker for PROTAC synthesis[1].
T18445 N-Methyl-N'-(azido-PEG2-C5)-Cy5 N-Methyl-N'-(azido-PEG2-C5)-Cy5 is a polyethylene glycol (PEG)-based linker that incorporates an azide functionality. This linker is primarily utilized in the synthesis of proteolysis targeting chimeras (PROTACs)[1].
T17680 Boc-NH-PEG4-Ms Boc-NH-PEG4-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.
T15955 Mal-Amido-PEG4-Boc Mal-Amido-PEG4-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.
T17628 Bis-PEG25-TFP ester Bis-PEG25-TFP 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.
T18519 PC-Biotin-PEG4-NHS carbonate PC-Biotin-PEG4-NHS carbonate is a polyethylene glycol (PEG) derived linker employed for the synthesis of proteolysis-targeting chimeras (PROTACs)[1].
T18570 Propargyl-PEG13-acid Propargyl-PEG13-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.
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