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E3 ligase ligands bind ubiquitin ligases such as cereblon and von Hippel-Lindau (VHL) in degrader design. In a degrader, they anchor the ligase end of the molecule. E3 ubiquitin ligases transfer ubiquitin to substrate proteins and mark them for degradation by the proteasome. Thalidomide and its analogs bind cereblon (CRBN), a substrate receptor of a cullin-based E3 ligase complex identified as their direct target in 2010. The category includes cereblon ligands such as thalidomide fluoride and TD-106, and VHL ligands such as VL285 and VH032-cyclopropane-F. These ligands are used to build proteolysis-targeting chimeras (PROTACs) and to study how ligases are recruited to new substrates.
ALAPYIP is a specific ligand for E3 ubiquitin ligase, effectively recruiting the VHL-E3 ligase. This compound plays a critical role in ubiquitination processes and can be utilized in the synthesis of FPP29. ALAPYIP is valuable for research aimed at understanding protein degradation pathways and the regulation of cellular processes through controlled ubiquitin signaling.
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E3 Ligase Ligand 50 is a specific ligand for the E3 ubiquitin ligase Cereblon. This compound facilitates the synthesis of proteolysis-targeting chimeras (PROTACs), specifically the BTK Degrader-10. It serves as a valuable tool in research applications focused on targeted protein degradation and therapeutic interventions in various diseases.
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DCAF11 ligand 1 is a specific ligand for the E3 ubiquitin ligase DCAF11. This compound is instrumental in the synthesis of PROTACs, specifically in the development of FF2039. Its utility in drug discovery and research applications makes it valuable for studies involving targeted protein degradation mechanisms.
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(S,R,S)-AHPC-Ac is a ligand for E3 ubiquitin ligases, facilitating the ubiquitination process crucial for protein degradation. This compound is instrumental in the development of PROTACs, such as SMARCA2/4-degrader-22, and is utilized in research focusing on targeted protein degradation mechanisms. Its role in modulating E3 ligase activity makes it valuable for studies in cellular signaling and protein homeostasis.
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(S,S,S)-VH032-cyclopropane-F is a ligand that targets E3 ubiquitin ligases, facilitating the selective degradation of specific proteins through the ubiquitin-proteasome system. This compound can be conjugated to target protein ligands using a linker to generate PROTAC derivatives, such as cis-VZ185, which are valuable tools for studying protein dynamics and cellular functions. Its unique mechanism provides opportunities for innovative research in targeted protein degradation and therapeutic development.
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E3 Ligase Ligand 33 (56-9B) acts as a ligand for E3 ubiquitin ligases, facilitating the ubiquitination process crucial for protein degradation and regulation. This compound is particularly valuable in anti-cancer research, where modulation of protein turnover can influence tumor progression and cell survival. Its application in target identification and pathway analysis makes it an essential tool for advancing understanding of ubiquitin-mediated signaling.
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(S,R,S)-AHPC-O-CF3 serves as a ligand for E3 ubiquitin ligases, facilitating targeted protein degradation through the ubiquitin-proteasome system. This compound can be utilized in the synthesis of PROTAC SMARCA2/4-degrader-20, which is instrumental for studying the modulation of SMARCA2 and SMARCA4 proteins. Its applications extend to research involving targeted therapy and novel drug development strategies in cancer and other diseases.
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Synonyms: VH032-NH2 dihydrochloride; VHL ligand 1 dihydrochloride
(S,R,S)-AHPC dihydrochloride is a VH032-based ligand that facilitates the recruitment of the von Hippel-Lindau (VHL) protein. This compound can be conjugated to various target proteins, such as BCR-ABL1, using a linker to create PROTACs like GMB-475. GMB-475 demonstrates significant biological activity by inducing degradation of BCR-ABL1, exhibiting an IC50 of 1.11 μM in Ba/F3 cells. This compound is valuable for research in targeted protein degradation and therapeutic development.
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Pomalidomide 7'OMe is a potent CRBN ligand that functions as an E3 ligase recruiter, facilitating the targeted degradation of proteins through the ubiquitin-proteasome pathway. Its unique structure allows for the potential linkage to BRD9 ligands, making it an essential component in the synthesis of PROTAC BRD9 degrader-9. This compound is valuable for research applications in targeted protein degradation and cellular signaling pathways.
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CRBN ligand-190 is a ligand for the CRBN-type E3 ubiquitin ligase, facilitating the targeted ubiquitination and degradation of proteins. This compound is instrumental in the development of PROTACs (proteolysis-targeting chimeras), notably for synthesizing PROTAC HPK1 Degrader-7. Its utility in protein degradation strategies makes it a valuable tool for research in targeted therapy and protein homeostasis.
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E3 Ligase Ligand 43 functions as a ligand for E3 ubiquitin ligase ACBI3. This compound is essential for the synthesis of Proteolysis Targeting Chimeras (PROTACs), allowing for targeted protein degradation. Its application is significant in cellular studies investigating protein turnover, signaling pathways, and disease mechanisms.
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E3 ligase Ligand 7 is a selective ligand for E3 ligase, facilitating targeted protein degradation through the formation of PROTACs (proteolysis-targeting chimeras). This compound serves as a key building block for the synthesis of PROTAC BET Degrader-12, enabling researchers to study the modulation of BET protein functions. E3 ligase Ligand 7 is valuable for applications in drug discovery and development, particularly in exploring therapeutic strategies for diseases associated with aberrant protein levels.
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VHL-SF2 is a selective ligand for the von Hippel-Lindau (VHL) protein, facilitating the synthesis of PROTACs (proteolysis-targeting chimeras). By engaging the VHL E3 ubiquitin ligase, VHL-SF2 promotes the targeted degradation of specific proteins, making it a valuable tool in drug discovery and development. This compound is essential for researchers investigating targeted protein degradation and enhancing the therapeutic potential of protein-based treatments.
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CRBN ligand-1 is a selective ligand for the E3 ubiquitin ligase cereblon (CRBN). This compound plays a critical role in mediating protein degradation through the ubiquitin-proteasome pathway, making it an important tool for studying protein homeostasis and cellular signaling mechanisms. It is utilized in research applications focused on targeted protein degradation and the development of novel therapeutics for diseases related to dysregulated protein dynamics.
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cIAP1 ligand 4 is an E3 ligase ligand designed for the synthesis of proteolysis-targeting chimeras (PROTACs). This compound facilitates the targeted degradation of proteins by engaging the cellular ubiquitin-proteasome system. Its application in molecular biology research allows for advanced manipulation of protein levels, enhancing studies related to protein function and cellular signaling pathways.
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E3 ligase Ligand 49 is an E3 ubiquitin ligase ligand that plays a critical role in the development of PROTAC (Proteolysis Targeting Chimeras) technology. This compound is specifically designed for the synthesis of PROTACs targeting XPO1, facilitating targeted protein degradation in various biological contexts. Its application is particularly relevant in studies focusing on protein regulation and degradation pathways, providing valuable insights into cellular processes and disease mechanisms.
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Pomalidomide-6-O-CH3 is a modified derivative of Pomalidomide that serves as a ligand for the E3 ubiquitin ligase cereblon (CRBN). This compound plays a crucial role in the recruitment of CRBN, facilitating targeted protein degradation through the formation of PROTACs when linked to other protein ligands. Its application in the study of protein turnover and degradation pathways makes it a valuable tool in chemical biology and therapeutic research.
E3 Ligase Ligand 29 serves as a ligand for E3 ligases, facilitating the ubiquitination process by targeting specific substrates for proteasomal degradation. This compound plays a crucial role in modulating cellular protein levels and has significant applications in research focused on protein homeostasis, cancer biology, and signal transduction pathways. The ability to selectively influence E3 ligase activity makes it a valuable tool for studying ubiquitin-mediated mechanisms.
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Dihydrouracil-Ph-2-Me-piperidine serves as a ligand for E3 ligase, facilitating targeted protein degradation through the PROTAC technology. It is instrumental in synthesizing the PROTAC HPK1 Degrader-6, which can be employed in studies aimed at modulating cellular pathways by specifically degrading target proteins. This compound is valuable for researchers investigating the therapeutic potential of PROTACs and E3 ligase-mediated protein degradation in various biological contexts.
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Thalidomide-C4-N2-C2-N3 is a potent E3 ligase ligand that facilitates the formation of PROTAC molecules. This compound is designed to bind to target protein ligands through a flexible linker, enabling the degradation of specific substrates such as sEH via the PROTAC mechanism. Its ability to modulate protein levels provides valuable utility in research applications focused on targeted protein degradation and therapeutic potential in various disease contexts.
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CRBN ligand-181 is an E3 ubiquitin ligase ligand designed to engage the cereblon (CRBN) target. This compound serves as a key building block for the development of proteolysis-targeting chimeras (PROTACs), enabling targeted degradation of specific proteins within cellular systems. Its application in research facilitates the study of targeted protein degradation and modulation of cellular pathways.
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CRBN ligand-200 is a ligand for the E3 ubiquitin ligase cereblon (CRBN) that facilitates the recruitment of the cereblon protein. This compound can be conjugated to a target protein ligand through a linker to create a PROTAC (Proteolysis Targeting Chimera), enabling targeted degradation of specific proteins. Research applications include studying protein turnover processes and developing novel therapeutic strategies in targeted protein degradation.
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CRBN ligand-625 is a selective ligand for the E3 ubiquitin ligase cereblon (CRBN), designed to facilitate the recruitment of CRBN to specific target proteins. This compound can be utilized in the development of proteolysis-targeting chimeras (PROTACs), enabling the selective degradation of proteins of interest. CRBN ligand-625 is essential for research in targeted protein degradation and protein homeostasis studies.
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CRBN ligand-363 is a specific ligand for the E3 ubiquitin ligase cereblon (CRBN), facilitating the recruitment of the CRBN protein. This compound can be conjugated to target protein ligands through a linker to create PROTACs, enabling targeted protein degradation. It serves as a valuable tool in research applications involving protein modulation and degradation pathways.
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CRBN ligand-557 is a ligand for the E3 ubiquitin ligase cereblon (CRBN), facilitating the recruitment of the CRBN protein. This compound can be utilized in conjunction with a target protein ligand via a linker to create proteolysis-targeting chimeras (PROTACs). It serves a crucial role in targeted protein degradation research, enabling the study of protein modulation and therapeutic interventions in various biological contexts.
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