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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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). |