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 | |
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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]. |