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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.
E3 Ligase Ligand 34 is an E3 ligase ligand that facilitates targeted protein degradation through the development of PROTACs. This compound is integral to the synthesis of PROTAC SMARCA2/4-degrader-35, enabling the selective degradation of SMARCA2 and SMARCA4 proteins. Its application in research supports the exploration of protein homeostasis and regulation pathways within cellular processes.
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MEL23 is an MDM2 E3 ligase inhibitor that specifically targets the E3 ligase activity of the MDM2-MDMX complex. This compound effectively inhibits the ubiquitination of MDM2 and p53, leading to decreased viability in cells expressing wild-type p53. Additionally, MEL23 stabilizes MDM2 through a mechanism that does not involve p53 transcription, making it a valuable tool for research into cancer biology and therapeutic strategies targeting the p53 pathway.
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E3 Ligase Ligand 75 is a ligand designed to selectively engage E3 ubiquitin ligases. This compound plays a pivotal role in the development of proteolysis-targeting chimeras (PROTACs), including the synthesis of K-Ras Degrader-7. It facilitates targeted protein degradation, making it a valuable tool in studies of protein regulation and therapeutic applications in cancer research.
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RR-11055 is a ligand for the E3 ligase cereblon, demonstrating a binding affinity with a Ki value of 0.38 μM. This compound is instrumental in the synthesis of PROTAC degrader ERD-1233, making it valuable for research in targeted protein degradation and modular drug design. Its ability to interact with E3 ligases positions RR-11055 as a significant tool for studying ubiquitin-mediated proteolysis.
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(S)-(S,R,S,R)-AHPC-Me-N3 is an E3 ligase ligand that facilitates targeted protein degradation through the synthesis of PROTAC molecules. It plays a crucial role in the development of PROTAC SMARCA2 degrader-32, enabling precise modulation of protein levels in cellular systems. This compound is valuable for researchers focused on protein degradation therapies and E3 ligase research.
N-Boc-SBP-0636457-OH is a ligand specifically targeting E3 ubiquitin ligases, facilitating the recruitment of IAP E3 ligases. This compound can be conjugated with Bcl-xL ligands via a linker to create the PROTAC Bcl-xL degrader-1, advancing research in targeted protein degradation and therapeutic applications in cancer biology. Its utility in the development of bifunctional molecules positions it as a valuable tool for studying protein homeostasis and signaling pathways.
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E3 Ligase Ligand 77 is a ligand targeting the CRBN type E3 ubiquitin ligase. This compound facilitates the synthesis of PROTACs, including PROTAC RET Degrader 1. Its primary application is in the development of targeted protein degradation strategies, enabling researchers to investigate and manipulate protein levels in various biological contexts. E3 Ligase Ligand 77 serves as a valuable tool in cellular and molecular biology studies.
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E3 Ubiquitin Ligase Binder-1 is a targeted ligand for E3 ubiquitin ligases, exhibiting potent binding affinity. This compound has significant implications in studies of protein degradation pathways and ubiquitination processes. It is especially useful in research focused on cellular signaling, protein homeostasis, and disease mechanisms related to ubiquitin-mediated proteolysis.
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Thalidomide-methylpyrrolidine is a ligand for E3 ubiquitin ligases, serving as an important tool in the study of protein degradation pathways. This compound has potential applications in research focused on cellular signaling, proteostasis, and the modulation of the ubiquitin-proteasome system. Additionally, it can be utilized as a precursor in the synthesis of CW-3308, facilitating further investigation into its biological effects.
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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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