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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-644 is a ligand for the E3 ubiquitin ligase cereblon (CRBN), facilitating the recruitment of this protein to target substrates. It can be conjugated to target protein ligands through a linker to generate a PROTAC (proteolysis-targeting chimera), enabling targeted protein degradation. This reagent is valuable for research in protein dynamics and therapeutic development through modulation of the ubiquitin-proteasome system.
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CRBN ligand-718 is a ligand for the E3 ubiquitin ligase cereblon (CRBN), facilitating the recruitment of the CRBN protein in cellular assays. This compound serves as a valuable tool for the development of proteolysis-targeting chimeras (PROTACs) by linking to a target protein ligand via a linker. Its applications include studying protein degradation pathways and creating innovative therapeutic strategies in targeted protein degradation research.
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CRBN ligand-295 is a selective ligand for the E3 ubiquitin ligase cereblon (CRBN). This compound facilitates the recruitment of CRBN to target proteins, enabling targeted protein degradation through the formation of proteolysis-targeting chimeras (PROTACs). It is ideal for research applications in drug discovery and development, particularly in the study of protein homeostasis and cellular regulation.
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CRBN ligand-290 is a selective ligand for the E3 ubiquitin ligase cereblon (CRBN), facilitating the recruitment of CRBN to target proteins. This compound serves as a building block for the development of PROTACs (Proteolysis Targeting Chimeras) by enabling the conjugation of CRBN with a target protein ligand through a suitable linker. Its application is significant in studies involving targeted protein degradation, offering insights into therapeutic interventions and functional protein regulation in various biological contexts.
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SJ6145 is a potent ligand for KLHDC2, exhibiting a dissociation constant (Kd) of 16.9 μM as determined by surface plasmon resonance (SPR) assays. This compound demonstrates an IC50 value of 42 μM in inhibiting KLHDC2's binding to a di-Gly degron peptide, highlighting its potential role in investigating KLHDC2-mediated cellular processes. SJ6145 can be utilized in research applications focused on protein degradation and regulatory mechanisms in cellular homeostasis.
CRBN ligand-629 is a ligand for the E3 ubiquitin ligase cereblon (CRBN), facilitating the recruitment of cereblon to specific target proteins. This compound can be employed in the design of PROTACs (PROteolysis-TArgeting Chimeras) by linking it to a target protein ligand through a suitable linker. Its application in targeted protein degradation makes it a valuable tool for researchers investigating novel therapeutic approaches in cancer and other diseases.
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CRBN ligand-637 is a ligand for the E3 ubiquitin ligase cereblon (CRBN), facilitating the recruitment of the cereblon protein in targeted protein degradation applications. This compound can be conjugated with a target protein ligand through a linker to create a PROTAC (proteolysis-targeting chimera), enabling the selective degradation of specific proteins. Its use in research may aid in elucidating mechanisms of protein regulation and disease pathways.
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CRBN ligand-386 functions as 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 using a linker to create a proteolysis-targeting chimera (PROTAC). Its ability to adapt and selectively induce protein degradation makes it a valuable tool in chemical biology and therapeutic research, particularly in studying targeted protein degradation mechanisms.
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CRBN ligand-689 is a ligand for the E3 ubiquitin ligase cereblon (CRBN), facilitating the engagement of CRBN with target proteins. This compound can be utilized in the development of PROTACs (proteolysis-targeting chimeras) by linking to a target protein ligand through a suitable linker. Its design is aimed at enhancing targeted protein degradation, making it a valuable tool for research in cellular signaling and therapeutic applications.
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CRBN ligand-112 is a selective ligand for the CRBN-type E3 ubiquitin ligase, serving as a critical component in the development of proteolysis-targeting chimeras (PROTACs). This compound facilitates the ubiquitination and subsequent degradation of target proteins, offering a powerful tool for investigating cellular protein turnover and modulation. Its application in research spans various fields, including cancer therapy and targeted protein degradation studies.
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CRBN ligand-482 is a potent ligand for the E3 ubiquitin ligase cereblon (CRBN), facilitating the recruitment of this protein in cellular processes. It serves as a crucial component for the development of PROTACs (proteolysis-targeting chimeras) by creating a linkage between a target protein ligand and cereblon. This compound is valuable for research applications focused on targeted protein degradation and the modulation of protein levels within cells.
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CRBN ligand-74 is a potent ligand for the CRBN E3 ubiquitin ligase, facilitating the development of PROTAC (Proteolysis Targeting Chimeras). It serves as a valuable tool in targeted protein degradation research, enabling the selective degradation of intracellular proteins. This compound is instrumental in studying various biological processes and therapeutic applications related to protein homeostasis.
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Desamino lenalidomide-4-Br-5-F is a potent ligand for the E3 ubiquitin ligase cereblon (CRBN), facilitating the recruitment of the cereblon protein. This compound can be utilized to create PROTACs (proteolysis-targeting chimeras) by linking it to a target protein ligand through a suitable linker. Its ability to modulate protein degradation makes it valuable in various research applications, including targeted protein elimination and the study of cellular mechanisms involving ubiquitin-proteasome pathways.
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CRBN ligand-568 is a ligand for the E3 ubiquitin ligase cereblon (CRBN), facilitating the recruitment of CRBN to specific target proteins. This compound can be equipped with a linker to create a PROTAC (proteolysis-targeting chimeras), enabling targeted protein degradation. CRBN ligand-568 is beneficial for studying protein regulation and ubiquitination processes in various biological contexts.
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CRBN ligand-375 is a ligand for the E3 ubiquitin ligase cereblon (CRBN), facilitating the recruitment of the CRBN protein. This compound can be conjugated with target-specific ligands through a linker to construct proteolysis-targeting chimeras (PROTACs). It is useful in studies aimed at modulating protein degradation pathways and investigating the role of CRBN in cellular processes.
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CRBN ligand-16 is a ligand for the E3 ubiquitin ligase CRBN, enabling targeted protein degradation through the formation of PROTAC molecules. This compound facilitates the ubiquitination and subsequent proteasomal degradation of specific proteins, offering valuable applications in drug development and disease research. Its utility in creating bifunctional degradation agents makes it a crucial tool for studies involving protein modulation and therapeutic interventions.
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CRBN ligand-427 is a ligand for the E3 ubiquitin ligase cereblon (CRBN), facilitating the recruitment of the CRBN protein to target proteins. This compound can be conjugated to a target protein ligand via a linker, enabling the formation of a PROTAC, a powerful tool for targeted protein degradation studies. Its application in protein modulation makes it valuable for various research avenues in therapeutic discovery and cellular biology.
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CRBN ligand-84 is a ligand for the CRBN-type E3 ubiquitin ligase, facilitating the ubiquitination process through targeted protein degradation. This compound is integral in the design and synthesis of PROTAC molecules, enabling the selective elimination of unwanted proteins in cellular studies. Its utility in research applications extends to investigating protein turnover and degradation pathways, supporting drug discovery efforts in targeted therapies.
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CRBN ligand-574 is a ligand for the E3 ubiquitin ligase cereblon (CRBN), facilitating the targeted recruitment of the cereblon protein. This compound can be utilized to create PROTACs by linking it to a target protein ligand through a suitable linker. Researchers can employ CRBN ligand-574 in studies aimed at exploring targeted protein degradation pathways and therapeutic development in various disease models.
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CRBN ligand-352 is a selective ligand for the E3 ubiquitin ligase cereblon (CRBN), facilitating the recruitment of CRBN to target proteins. This compound can be conjugated to target protein ligands through a suitable linker, enabling the development of PROTACs (proteolysis-targeting chimeras). Its application in targeted protein degradation research provides a valuable tool for studying protein function and modulation in cellular pathways.
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CRBN ligand-662 is a selective ligand for the E3 ubiquitin ligase cereblon (CRBN), facilitating the recruitment of the cereblon protein. This compound can be conjugated to a target protein ligand through a linker to generate a PROTAC (proteolysis-targeting chimera). Its utility in targeted protein degradation research makes it a valuable tool for studying cellular protein regulation and potential therapeutic applications.
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CRBN ligand-627 is a specific 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 PROTAC (proteolysis-targeting chimera), enabling selective degradation of target proteins. It serves as a valuable tool in chemical biology and therapeutic research, particularly in the development of targeted protein degradation strategies.
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CRBN ligand-440 is a potent ligand for the E3 ubiquitin ligase cereblon (CRBN), facilitating the recruitment of this protein within cellular systems. Its design allows for conjugation with target protein ligands through a linker, enabling the synthesis of proteolysis-targeting chimeras (PROTACs). This compound is valuable for studying protein degradation pathways and exploring novel therapeutic strategies in targeted protein degradation research.
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CRBN ligand-543 targets the E3 ubiquitin ligase cereblon (CRBN) and is utilized for its ability to recruit the CRBN protein. This compound can be conjugated to a target protein ligand through a linker to create a Proteolysis Targeting Chimera (PROTAC), facilitating targeted protein degradation. Research applications include the investigation of protein modulation and therapeutic strategies in various diseases.
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CRBN ligand-717 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 generate a PROTAC (proteolysis-targeting chimera), thereby enabling targeted protein degradation. It is valuable in research applications focused on protein regulation and degradation pathways.
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