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 | |
---|---|---|
T14401 | Azido-C2-SS-PEG2-C2-acid | Azido-C2-SS-PEG2-C2-acid is a two-unit cleavable PEG linker employed in the synthesis of antibody-drug conjugates (ADCs) [1]. |
T17122 | Tos-PEG2-C2-Boc | Tos-PEG2-C2-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. |
T14607 | Biotin-PEG6-alcohol | Biotin-PEG6-alcohol is a PEG-based PROTAC linker containing a biotin label. This compound serves as a key component in the synthesis of PROTACs, facilitating the conjugation of target-recruiting moiety and E3 ligase-recruiting moiety [1]. |
T17748 | DBCO-CONH-S-S-NHS ester | DBCO-CONH-S-S-NHS ester is a disulfide-linked ADC linker employed for the synthesis of antibody-drug conjugates (ADCs)[1]. |
T17781 | DBCO-PEG10-DBCO | DBCO-PEG10-DBCO 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. |
T17373 | Ald-Ph-PEG12-TFP ester | Ald-Ph-PEG12-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. |
T17896 | cIAP1 Ligand-Linker Conjugates 4 | cIAP1 Ligand-Linker Conjugates 4 is a chemical compound that comprises an IAP ligand specifically designed for the E3 ubiquitin ligase and a PROTAC linker. This compound, cIAP1 Ligand-Linker Conjugates 4, has the potential to be utilized in the development of SNIPERs[1]. |
T17944 | Fluorescein-PEG5-NHS ester | Fluorescein-PEG5-NHS ester, a PEG-based PROTAC linker, facilitates PROTAC synthesis[1]. |
T18302 | Mal-Phe-C4-VC-PAB-DMEA-PNU-159682 | Mal-Phe-C4-VC-PAB-DMEA-PNU-159682 is a drug-linker conjugate utilized in antibody-drug conjugate (ADC) therapy. It comprises the ADC linker Mal-Phe-C4-VC-PAB and the potent ADC cytotoxin DMEA-PNU-159682. DMEA-PNU-159682 encompasses metabolites of nemorubicin (MMDX) derived from liver microsomes, as well as the ADC cytotoxin PNU-159682[1]. |
T14696 | BnO-PEG1-CH2CO2tBu | BnO-PEG1-CH2CO2tBu 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. |
T14719 | Boc-Aminooxy-PEG4-NH2 | Boc-Aminooxy-PEG4-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. |
T17702 | Bromoacetamido-PEG9-ethylcarbamoyl-C12-Boc | Bromoacetamido-PEG9-ethylcarbamoyl-C12-Boc is a polyethylene glycol (PEG) derived linker employed for synthesizing proteolysis-targeting chimeras (PROTACs)[1]. |
T17125 | Tos-PEG2-O-Propargyl | Tos-PEG2-O-Propargyl is a polyethylene glycol (PEG)-based proteolysis targeting chimera (PROTAC) linker, commonly employed for the synthesis of Thalidomide-O-PEG2-propargyl[1]. |
T17390 | Amine-PEG-amine (MW 2000) | Amine-PEG-amine (MW 2000) is a polyethylene glycol (PEG) derivative that functions as a linker for PROTAC synthesis. PROTACs are small molecules used for targeted protein degradation [1]. |
T16618 | Propargyl-PEG4-Boc | Propargyl-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. |
T14420 | Azido-PEG2-C2-sulfonic acid | Azido-PEG2-C2-sulfonic acid is a polyethylene glycol (PEG) derived linker compound employed for the synthesis of proteolysis-targeting chimeras (PROTACs) [1]. |
T18294 | Mal-PEG4-VC-PAB-DMEA | Mal-PEG4-VC-PAB-DMEA is a cleavable ADC linker that incorporates a Maleimide moiety. It is employed in the synthesis of antibody-drug conjugates (ADCs)[1]. |
T18145 | m-PEG13-Boc | m-PEG13-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. |
T17787 | DBCO-PEG2-NH-Boc | DBCO-PEG2-NH-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. |
T14113 | Acid-PEG9-NHS ester | Acid-PEG9-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. |