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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.
CRBN ligand-376 is a potent ligand for the E3 ubiquitin ligase cereblon (CRBN), facilitating the recruitment of the CRBN protein. This compound can be utilized in the development of PROTACs by linking it to a target protein ligand through a suitable linker. Its application in targeted protein degradation provides valuable tools for elucidating protein functions and advancing therapeutic strategies.
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CRBN ligand-552 is a selective ligand for the E3 ubiquitin ligase cereblon (CRBN). It facilitates the recruitment of the CRBN protein, enabling the targeted degradation of specific proteins in cellular systems. This compound can be utilized in the design of PROTACs (proteolysis-targeting chimeras) by linking it to a target protein ligand through a suitable linker, making it a valuable tool in drug discovery and development.
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CRBN ligand-511 is a selective ligand for the E3 ubiquitin ligase cereblon (CRBN), facilitating the targeted recruitment of CRBN. This compound can be conjugated to target protein ligands through a linker to create proteolysis-targeting chimeras (PROTACs). Its application in degrading specific proteins makes it a valuable tool in chemical biology and therapeutic development for modulating cellular pathways.
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CRBN ligand-359 is a specialized ligand for the E3 ubiquitin ligase cereblon (CRBN), enabling the recruitment of the cereblon protein for targeted degradation. This compound can be conjugated to a target protein ligand through a linker to construct a PROTAC, facilitating the selective modulation of protein levels in cellular studies. Its application in protein degradation research makes it a valuable tool for investigating protein function and developing novel therapeutic strategies.
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CRBN ligand-111 acts as a ligand for the CRBN E3 ubiquitin ligase, facilitating targeted protein degradation through PROTAC (proteolysis-targeting chimeras) technology. This compound is vital for research focused on the modulation of ubiquitin-proteasome pathways, enabling the selective degradation of proteins involved in various cellular processes. Its application is particularly significant in studies aimed at therapeutic development, including cancer biology and neurodegenerative diseases.
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5-(2-Chloroacetamide) thalidomide is a Thalidomide analog that functions as an E3 ligase recruiter, facilitating the ubiquitination and targeted degradation of specific proteins. The inclusion of a chloroacetamide moiety enhances its reactivity towards thiol groups, potentially increasing its efficacy in modulating protein degradation pathways. This compound is of interest for research applications in targeted protein therapy and cancer biology, providing insights into the mechanisms of protein homeostasis.
VHL Ligand 35 is a selective ligand of the von Hippel-Lindau protein (pVHL) E3 ubiquitin ligase with a dissociation constant (Kd) of 0.291 μM. This compound effectively disrupts the protein-protein interaction between pVHL and hypoxia inducible factor 1α (HIF-1α), which is critical for regulating cellular responses to hypoxia. VHL Ligand 35 is valuable for research applications involving hypoxia signaling pathways and cancer biology, particularly in studies targeting the mechanisms of HIF regulation.
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CRBN ligand-366 is a ligand for the E3 ubiquitin ligase cereblon (CRBN), facilitating the recruitment of CRBN to target proteins. This compound can be conjugated with a target protein ligand through a linker, enabling the formation of a PROTAC (Proteolysis Targeting Chimera). Its utility in protein degradation strategies makes it valuable for research in protein homeostasis and targeted therapeutics.
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CRBN Ligand-723 is an efficient ligand targeting the E3 ubiquitin ligase cereblon (CRBN). This compound facilitates the recruitment of the cereblon protein and is designed to be conjugated to a target protein ligand through a linker to create a PROTAC (proteolysis-targeting chimera). It is valuable for research applications involving targeted protein degradation and cellular signaling pathways.
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CRBN ligand-458 is a ligand for the E3 ubiquitin ligase cereblon (CRBN), facilitating the recruitment of the cereblon protein. This compound is designed for use in the development of Proteolysis Targeting Chimeras (PROTACs) by linking to target protein ligands through a suitable linker. Its application enables targeted degradation of specific proteins, providing valuable tools for research in cancer biology and drug discovery.
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CRBN ligand-522 is a ligand for the E3 ubiquitin ligase cereblon (CRBN), serving as a tool for targeted protein degradation. It facilitates the recruitment of cereblon to specific target proteins through a linking mechanism, enabling the formation of PROTACs (proteolysis-targeting chimeras). This compound is valuable for research applications aimed at elucidating the role of targeted degradation in cellular processes and for drug discovery strategies focusing on protein modulation.
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Desamino lenalidomide-6-C-COOH is a ligand for E3 ubiquitin ligase cereblon (CRBN), facilitating the recruitment of the cereblon protein in biochemical assays. This compound can be conjugated with a target protein ligand through a linker to create a proteolysis-targeting chimera (PROTAC), enabling targeted protein degradation. Its applications in drug development and cellular studies enhance understanding of protein regulation and therapeutic strategies.
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CRBN ligand-76 is a ligand for the CRBN E3 ubiquitin ligase, facilitating the development of PROTAC (Proteolysis Targeting Chimeras). This compound engages specifically with the CRBN E3 ligase, promoting ubiquitination and degradation of target proteins. Its application in targeted protein degradation offers potential for therapeutic intervention in various diseases, including cancer and neurodegenerative disorders.
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CRBN ligand-148 is an E3 ubiquitin ligase ligand specifically targeting cereblon (CRBN). This compound facilitates the development of proteolysis-targeting chimeras (PROTACs) by promoting the ubiquitination and subsequent degradation of target proteins. Its biological activity is leveraged in research focused on targeted protein degradation and the modulation of cellular pathways.
CRBN ligand-606 is a potent ligand for the E3 ubiquitin ligase cereblon (CRBN). This compound facilitates the recruitment of the CRBN protein, enabling targeted protein degradation through the formation of PROTACs when linked to specific target protein ligands. It is particularly useful in the study of protein homeostasis and degradation pathways, making it valuable for various research applications in cellular biology and therapeutic development.
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CRBN ligand-298 is a ligand for the E3 ubiquitin ligase cereblon (CRBN), enabling the selective recruitment of CRBN to target proteins. By facilitating the formation of a PROTAC (proteolysis-targeting chimera), CRBN ligand-298 functions to promote targeted protein degradation, making it a valuable tool for studies in protein regulation and therapeutic development. This reagent is essential for researchers investigating the therapeutic potential of targeted protein degradation pathways.
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CRBN ligand-371 is a ligand for the E3 ubiquitin ligase cereblon (CRBN), facilitating the recruitment of the CRBN protein. This compound can be conjugated to a target protein ligand through a linker to create a proteolysis-targeting chimera (PROTAC). CRBN ligand-371 is useful in studies involving targeted protein degradation and the modulation of cellular pathways.
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CRBN ligand-570 is a selective ligand for the E3 ubiquitin ligase cereblon (CRBN) that facilitates the recruitment of the cereblon protein to target proteins. This compound can be utilized in the design of Proteolysis Targeting Chimeras (PROTACs) by linking it to specific target protein ligands through an appropriate linker. It is a valuable tool for studying targeted protein degradation and the therapeutic potential of modulating protein levels within cellular systems.
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CRBN ligand-14 is a ligand targeting the CRBN E3 ubiquitin ligase, facilitating the formation of PROTACs (PROteolysis TArgeting Chimeras). This compound plays a crucial role in targeted protein degradation, enabling the selective elimination of proteins of interest within cellular systems. It is particularly valuable in drug discovery and development, providing insights into protein regulation and therapeutic interventions in various diseases.
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CRBN ligand-389 is a ligand for the E3 ubiquitin ligase cereblon (CRBN), facilitating the recruitment of the CRBN protein. This compound can be utilized in the development of proteolysis-targeting chimeras (PROTACs) by linking to target protein ligands through a suitable linker. The application of CRBN ligand-389 in research may aid in the modulation of protein degradation pathways and the exploration of targeted therapeutic strategies.
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CRBN ligand-735 is a ligand for the E3 ubiquitin ligase cereblon (CRBN), functioning to recruit the CRBN protein. This compound can be conjugated with a target protein ligand through a linker, facilitating the formation of a PROTAC (proteolysis-targeting chimera). CRBN ligand-735 is essential for research in targeted protein degradation and the development of novel therapeutic strategies that exploit the ubiquitin-proteasome system.
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(S,R,R)-VH032 hydrochloride is a selective ligand for the von Hippel-Lindau (VHL) E3 ligase. This compound facilitates the targeted degradation of proteins by enabling the formation of proteolysis-targeting chimeras (PROTACs) when conjugated to specific target protein ligands through a linker. Its unique mechanism allows for the modulation of cellular protein levels, making it a valuable tool in biochemical research and drug discovery applications.
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CRBN ligand-762 is a ligand for the E3 ubiquitin ligase cereblon (CRBN), facilitating the recruitment of this protein for ubiquitination processes. This compound can be conjugated with target protein ligands through a linker to create proteolysis-targeting chimeras (PROTACs). Its application in targeted protein degradation makes it a valuable tool for studying cellular mechanisms and therapeutic interventions.
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CRBN ligand-350 is a selective ligand for the E3 ubiquitin ligase cereblon (CRBN), facilitating the recruitment of the cereblon protein to target proteins. This compound is engineered for use in the development of Proteolysis Targeting Chimeras (PROTACs), enabling targeted protein degradation and therapeutic applications in various disease models. Its utility in chemical biology supports research aimed at elucidating protein interactions and regulatory mechanisms.
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CRBN ligand-545 is an E3 ubiquitin ligase cereblon (CRBN) ligand that effectively recruits the cereblon protein. This compound facilitates the development of proteolysis-targeting chimeras (PROTACs) by enabling linkages to target protein ligands via a suitable linker. Its application in targeted protein degradation research underscores its potential in therapeutic development for various diseases.
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