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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T17883 | Pomalidomide-PEG3-C2-NH2 | Pomalidomide-PEG3-C2-NH2 (Cereblon Ligand-Linker Conjugates 5) 是一种合成的 E3 连接酶配体-linker 偶联物,包含基于 Pomalidomide 的 cereblon 配体和 3 单元 PEG 的linker。 |
T17582 | DADPS Biotin Azide | DADPS Biotin Azide (Biotin-PEG4-amino-t-Bu-DADPS-C6-azide) 是一种属于 PEG 类的 PROTAC linker,可用于合成 PROTAC 分子。 |
T17015L | (S)-TCO-PEG4-acid | (S)-TCO-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. |
T17853 | DSPE-PEG-Maleimide (MW 5000) | DSPE-PEG-Maleimide (MW 5000) 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. |
T16603 | Propargyl-PEG2-OH | Propargyl-PEG2-OH is a polyethylene glycol (PEG)-based PROTAC linker, specifically designed for efficient synthesis of Thalidomide-O-PEG2-propargyl. |
T17670 | Boc-NH-PEG15-azide | Boc-NH-PEG15-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. |
T17718 | Cbz-NH-PEG10-CH2COOH | Cbz-NH-PEG10-CH2COOH 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. |
T18325 | MC-Val-Cit-PAB-Indibulin | MC-Val-Cit-PAB-Indibulin is an antitumor drug-linker conjugate for antibody-drug conjugates (ADCs), featuring the orally active tubulin assembly inhibitor, Indibulin, connected through the MC-Val-Cit-PAB ADC linker. This compound exhibits potent antitumor activity. |
T14182 | Alkyne-ethyl-PEG1-Boc | Alkyne-ethyl-PEG1-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. |
T15078 | DBCO-Sulfo-NHS ester sodium | DBCO-Sulfo-NHS ester sodium is a cleavable linker predominantly employed in the synthesis of antibody-drug conjugates (ADCs)[1]. |
T18349 | Methyltetrazine-PEG4-NH-Boc | Methyltetrazine-PEG4-NH-Boc is a PEGylation-based linker employed for synthesizing Proteolysis Targeting Chimeras (PROTACs)[1]. |
T18623 | Boc-NH-PEG2-C2-amido-C4-acid | Boc-NH-PEG2-C2-amido-C4-acid (PROTAC Linker 30) is a polyethylene glycol (PEG)-based linker utilized for the synthesis of Proteolysis Targeting Chimeras (PROTACs)[1]. |
T18164 | m-PEG24-NHS ester | m-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. |
T14771 | Br-PEG4-C2-Boc | Br-PEG4-C2-Boc is a cleavable 4-unit PEG ADC linker employed for the synthesis of antibody-drug conjugates (ADCs)[1]. |
T15297 | Fluorescein-thiourea-PEG2-azide | Fluorescein-thiourea-PEG2-azide is a PEG-derived linker commonly applied for the synthesis of PROTACs[1]. |
T15873 | m-PEG4-C6-phosphonic acid ethyl ester | m-PEG4-C6-phosphonic acid ethyl ester is a polyethylene glycol (PEG)-based linker compound utilized for synthesizing proteolysis-targeting chimeras (PROTACs)[1]. |
T17888 | cIAP1 Ligand-Linker Conjugates 6 hydrochloride | cIAP1 Ligand-Linker Conjugates 6 hydrochloride is a compound that combines an IAP ligand for the E3 ubiquitin ligase and a PROTAC linker. It is utilized for the purpose of designing SNIPERs[1]. |
T16637 | Propargyl-PEG6-NHS ester | Propargyl-PEG6-NHS ester is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1]. |
T14605 | Biotin-PEG5-NH-Boc | Biotin-PEG5-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. |
T18280 | Mal-PEG24-acid | Mal-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. |