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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
T17540 BCN-SS-NHS BCN-SS-NHS is a cleavable linker vital in ADC synthesis. BCN-SS-NHS joins cytotoxic drugs to antibodies, enabling precise delivery to cells or proteins. The cleavable nature ensures controlled drug release, optimizing ADC effectiveness.
T16207 N-Boc-N-bis(PEG4-azide) N-Boc-N-bis(PEG4-azide) is a PEG-based PROTAC linker employed for the synthesis of PROTACs[1].
T15476 Hexaethylene glycol Hexaethylene glycol 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.
T18737 AcLysValCit-PABC-DMAE-SW-163D AcLysValCit-PABC-DMAE-SW-163D is a drug-linker conjugate for antibody-drug conjugates (ADCs), featuring a natural bis-intercalator, SW-163D, attached through an AcLysValCitPABC-DMAE linker[1].
T14435 Azido-PEG3-Val-Cit-PAB-OH Azido-PEG3-Val-Cit-PAB-OH is a cleavable three-unit polyethylene glycol antibody-drug conjugate (ADC) linker utilized in ADC synthesis [1].
T17644 Boc-Aminooxy-PEG5-amine Boc-Aminooxy-PEG5-amine is a polyethylene glycol (PEG)-based PROTAC linker for the synthesis of PROTACs.
T17738 Cy5-PEG6-acid Cy5-PEG6-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.
T18413 N-Desthiobiotin-N-bis(PEG4-t-butyl ester) N-Desthiobiotin-N-bis(PEG4-t-butyl ester) is a PEG-based linker compound employed for the synthesis of PROTACs, which are bifunctional molecules designed for targeted protein degradation[1].
T15230 endo-BCN-PEG8-acid endo-BCN-PEG8-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.
T15294 Fluorescein-PEG5-acid Fluorescein-PEG5-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.
T14818 Bromoacetamido-PEG2-C2-NHS ester Bromoacetamido-PEG2-C2-NHS ester is a PEGylation-based linker compound utilized in PROTAC synthesis[1].
T18020 HS-PEG10-CH2CH2COOH HS-PEG10-CH2CH2COOH 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.
T18341 Methyltetrazine-PEG12-DBCO Methyltetrazine-PEG12-DBCO is a polyethylene glycol (PEG)-based linker compound utilized in the synthesis of proteolysis targeting chimeras (PROTACs)[1].
T16614 Propargyl-PEG4-acid Propargyl-PEG4-acid is a PEG-based PROTAC linker can be used in the synthesis of BTK-IAP PROTACs Ibrutinib -based PROTAC 2 and an analogue PROTAC 3. PROTAC 3 causes BTK degradation with a DC50 of 200 nM in THP-1 cells[1].
T14451 Azido-PEG4-NHS-ester Azido-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.
T15153 DNP-PEG4-alcohol DNP-PEG4-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.
T14640 Bis-PEG4-PFP ester Bis-PEG4-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.
T14801 Bromo-PEG4-acid Bromo-PEG4-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.
T17496 Azido-PEG24-acid Azido-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.
T18620 Tos-PEG2-NH2 Tos-PEG2-NH2 (PROTAC Linker 27) is a Polyethylene Glycol (PEG)-based linker used for the synthesis of Proteolysis-Targeting Chimeras (PROTACs)[1].
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