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 | |
---|---|---|
T17051 | Tetraethyl decane-1,10-diylbis(phosphonate) | Tetraethyl decane-1,10-diylbis(phosphonate) is an alkyl chain-derived linker for PROTACs synthesis[1]. |
T16298 | NH-bis(m-PEG8) | NH-bis(m-PEG8) 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. |
T17960 | Fmoc-N-PEG23-acid | Fmoc-N-amido-PEG23-acid is a polyethylene glycol (PEG)-based linker utilized for the synthesis of proteolysis-targeting chimeras (PROTACs)[1]. |
T17906 | Pomalidomide-amido-C4-amido-PEG2-C2-NH-Boc | Pomalidomide-amido-C4-amido-PEG2-C2-NH-Boc is a novel synthesized conjugate compound functioning as an E3 ligase ligand-linker in PROTAC technology. This compound incorporates a Pomalidomide-derived cereblon ligand, which binds selectively to the E3 ligase cereblon, and a 2-unit PEG linker, which provides stability and flexibility to the conjugate. |
T17470 | Azide-PEG6-amido-C16-Boc | Azide-PEG6-amido-C16-Boc is an alkyl/ether-based PROTAC linker utilized in PROTAC synthesis[1]. |
T17387 | Aloc-D-Ala-Phe-Lys(Aloc)-PAB-PNP | Aloc-D-Ala-Phe-Lys(Aloc)-PAB-PNP is a cleavable linker utilized in the synthesis of antibody-drug conjugates (ADCs), which are innovative therapeutic agents that combine the targeting ability of antibodies with potent cytotoxic drugs. |
T14736 | Boc-NH-PEG2-C2-NHS ester | Boc-NH-PEG2-C2-NHS ester is an alkyl/ether-derived PROTAC linker employed for the synthesis of PROTACs[1]. |
T15066 | DBCO-NHS ester 2 | DBCO-NHS ester 2 is a cleavable linker employed in the synthesis of antibody-drug conjugates (ADCs). It is a Dibenzylcyclooctyne (DBCO) derivative specifically designed for application in copper-free click chemistry [1]. |
T14788 | Bromo-PEG2-bromide | Bromo-PEG2-bromide 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. |
T17988 | Gly-Gly-Gly-PEG4-methyltetrazine | Gly-Gly-Gly-PEG4-methyltetrazine is a four-unit PEG ADC linker that is cleavable. It finds utility in the synthesis of antibody-drug conjugates (ADCs)[1]. |
T17450 | APN-PEG4-BCN | APN-PEG4-BCN is a cleavable four-unit polyethylene glycol (PEG) linker, employed in the synthesis of antibody-drug conjugates (ADCs)[1]. |
T15971 | Mal-NH-ethyl-SS-propionic acid | Mal-NH-ethyl-SS-propionic acid, a cleavable linker employed for the synthesis of antibody-drug conjugates (ADCs)[1], plays a crucial role in the modulation of drug release from the conjugate. |
T18197 | m-PEG37-hydrazide | m-PEG37-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. |
T17845 | DOTA-PEG5-C4-DBCO | DOTA-PEG5-C4-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. |
T18385 | N-(Azido-PEG4)-N-bis(PEG4-NHS ester) | N-(Azido-PEG4)-N-bis(PEG4-NHS ester), a PEG-based PROTAC linker, serves as a valuable component in the synthesis of PROTACs[1]. |
T18144 | m-PEG12-Thiol | m-PEG12-Thiol 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. |
T17556 | Biotin-PEG11-azide | Biotin-PEG11-azide 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. |
T17901 | cIAP1 Ligand-Linker Conjugates 10 | cIAP1 Ligand-Linker Conjugates 10 comprise of an IAP ligand and a PROTAC linker, which facilitates the design of SNIPERs. These conjugates incorporate an IAP ligand that interacts with the E3 ubiquitin ligase, and a PROTAC linker. SNIPERs can be developed using cIAP1 Ligand-Linker Conjugates 10. |
T17375 | Ald-Ph-PEG24-NHS ester | Ald-Ph-PEG24-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. |
T14108 | Acid-PEG5-C2-Boc | Acid-PEG5-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. |