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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-6-5-5-VHL is a potent and selective VHL-based PROTAC degrader targeting cereblon (CRBN), with a DC₅₀ of 1.5 nM. It selectively degrades CRBN without affecting neo-substrates IKZF1 and IKZF3.
Tz-Thalidomide is a tetrazine-tagged thalidomide derivative that functions as a ligand for E3 ligases. It exhibits binding affinity for BRD4, with IC₅₀ values of 46.25 μM for BRD4-1 and 62.55 μM for BRD4-2. As a click chemistry reagent, Tz-Thalidomide contains a tetrazine moiety capable of undergoing inverse electron demand Diels–Alder (iEDDA) reactions with trans-cyclooctene (TCO)-containing molecules, enabling bioorthogonal labeling and conjugation applications.
TD-165 is a PROTAC (proteolysis-targeting chimera) that targets cereblon (CRBN) for selective degradation of proteins. This compound features a CRBN ligand binding group, a linker, and a von Hippel-Landau (VHL) binding group, facilitating targeted ubiquitination and proteolytic degradation of specific proteins involved in cellular processes. TD-165 is suitable for research applications focused on targeted protein degradation, therapeutic development, and elucidating protein function in various biological contexts.
Synonyms: CC-90009
Eragidomide is a selective cereblon (CRBN) E3 ligase modulator that acts as a molecular glue, specifically targeting GSPT1 for ubiquitination. By co-opting the CRL4CRBN complex, Eragidomide facilitates the proteasomal degradation of GSPT1, leading to significant biological effects. This compound is primarily utilized in research applications focused on cancer biology and therapeutic strategies that exploit the proteasome pathway.
Thalidomide 5-fluoride is a thalidomide-derived ligand for the E3 ubiquitin ligase Cereblon, enabling targeted protein degradation via the PROTAC approach. This compound can be conjugated with specific target protein ligands, such as IRAK4, to create PROTAC molecules for enhanced therapeutic applications. Notably, PROTAC IRAK4 degrader-1 demonstrated significant IRAK4 protein degradation in OCI-LY-10 cells at concentrations of 0.01, 0.1, and 1 μM, achieving degradation levels of 20-50%, and >50%, respectively. This underlines its potential utility in cellular studies of protein regulation and targeted therapeutics.
Thalidomide-5-OH is an E3 ligase ligand that specifically targets the cereblon (CRBN) protein. This compound facilitates the recruitment of CRBN, enabling targeted protein degradation through the formation of PROTACs (proteolysis-targeting chimeras) by linking it to another ligand. Thalidomide-5-OH is utilized in research applications focusing on targeted protein degradation and therapeutic development for various diseases.
Thalidomide-NH-CH2-COOH is a Thalidomide-derived ligand that specifically targets the cereblon (CRBN) protein, facilitating its recruitment in various biological processes. This compound serves as a crucial building block for the development of PROTACs, allowing researchers to design targeted protein degradation strategies. Its application is significant in the study of protein homeostasis and the therapeutic potential of targeted protein modulation.
Thalidomide-propargyl is a thalidomide-derived ligand that selectively targets Cereblon (CRBN) for protein recruitment. This compound is instrumental in the development of immunomodulatory drug (IMiD) based PROTACs, facilitating targeted protein degradation. Additionally, Thalidomide-propargyl features an alkyne functional group, enabling it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc) reactions with azide-containing molecules, making it a valuable tool for click chemistry applications in chemical biology research.
Thalidomide-5,6-F is a Thalidomide-derived ligand that selectively targets cereblon (CRBN), facilitating its recruitment for the targeted degradation of specific proteins via the ubiquitin-proteasome pathway. This compound is instrumental in the development of PROTACs (proteolysis-targeting chimeras), enabling innovative approaches in the research of targeted protein degradation, drug discovery, and therapeutic interventions. Its unique mechanism offers valuable insights into cellular regulation and disease processes.
Thalidomide-5-COOH serves as a ligand for cereblon (CRBN), functioning through its interaction with the E3 ubiquitin ligase complex. This compound is instrumental in the development of PROTACs, enabling targeted protein degradation for potential therapeutic applications. Its role in bridging target proteins for ubiquitination makes it a valuable reagent in chemical biology and drug discovery research.
Thalidomide-O-C8-COOH is a Thalidomide-derived ligand targeting the E3 ligase Cereblon (CRBN). This compound facilitates the recruitment of CRBN protein, serving as a vital component for the development of Proteolysis Targeting Chimeras (PROTACs). Its unique structure allows for the effective conjugation with other ligands, enabling targeted protein degradation, making it an essential tool in chemical biology and therapeutic research.
Thalidomide-O-C8-Boc is a derivative of Thalidomide that functions as a ligand for the E3 ubiquitin ligase Cereblon (CRBN). This compound is utilized in the development of PROTACs by facilitating the recruitment of CRBN to target proteins through a linker. Its key biological activity involves modulating protein degradation pathways, making it valuable in drug discovery and therapeutic research targeting diseases linked to aberrant protein expressions.
Thalidomide-5-O-C4-NH2 hydrochloride is a potent ligand targeting the E3 ubiquitin ligase cereblon (CRBN). This compound facilitates the recruitment of CRBN, enabling the selective degradation of target proteins through the PROTAC (proteolysis-targeting chimera) mechanism. Thalidomide-5-O-C4-NH2 hydrochloride is instrumental in research applications focused on targeted protein degradation and the modulation of cellular pathways.
Cereblon inhibitor 2 is an effective inhibitor of the Cereblon protein, primarily targeting its role in regulating substrate degradation through the CRL4 E3 ubiquitin ligase complex. This compound exhibits significant biological activity in inhibiting cancer cell proliferation and enhancing apoptosis, making it a valuable tool in solid tumor research, particularly in breast cancer studies. Its application may facilitate advancements in understanding the molecular mechanisms underlying tumor biology and therapeutic resistance.
Thalidomide-NH-C9-NH2 hydrochloride serves as a ligand for the E3 ligase cereblon (CRBN). This compound facilitates the recruitment of CRBN, enabling targeted protein degradation. It can be conjugated to other ligands through a linker to create proteolysis-targeting chimeras (PROTACs), making it a valuable tool for research in the fields of targeted therapy and protein homeostasis.
Thalidomide-5-methyl functions as an E3 ligase ligand, specifically targeting cereblon (CRBN). This compound facilitates the recruitment of CRBN protein, enabling the development of PROTAC (proteolysis-targeting chimeras) for targeted protein degradation strategies. Thalidomide-5-methyl is a valuable tool in chemical biology and drug discovery research, particularly for studies related to targeted therapies and the modulation of protein stability.
Thalidomide-5-O-C2-NH2 hydrochloride is a ligand that targets cereblon, an E3 ubiquitin ligase, facilitating the recruitment of CRBN protein. This compound serves as an essential component in the development of PROTACs (proteolysis-targeting chimeras), enabling selective degradation of target proteins. Its unique mechanism allows researchers to explore the therapeutic potential of targeted protein degradation in various biological contexts, including cancer and other diseases.
Thalidomide-5-propargyl is a propargyl-modified derivative of Thalidomide that selectively targets Cereblon (CRBN). By recruiting CRBN proteins, this compound plays a significant role in the development of proteolysis-targeting chimeras (PROTACs). The presence of an alkynyl group enables its direct use in triazole synthesis, facilitating the creation of innovative PROTAC molecules designed for therapeutic applications.
Thalidomide-4-NH-PEG1-NH-Boc is a Boc-modified derivative of Thalidomide that serves as a ligand for the E3 ubiquitin ligase, Cereblon (CRBN). This compound is integral in PROTAC (proteolysis-targeting chimera) synthesis, allowing for efficient recruitment of CRBN to target proteins for degradation. The Boc protecting group can be removed under acidic conditions, facilitating further chemical modifications required in PROTAC development. Thalidomide-4-NH-PEG1-NH-Boc is an essential intermediate for researchers exploring targeted protein degradation and related therapeutic strategies.
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Thalidomide-5-NH-PEG2-NH2 hydrochloride serves as a ligand for E3 ligase, specifically targeting cereblon (CRBN) proteins. This compound facilitates the formation of PROTAC molecules by linking to a target protein, thereby promoting targeted protein degradation. Its applications extend to the study of protein modulation and degradation pathways in various cellular contexts, enhancing research in drug development and therapeutic strategies.
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Thalidomide-5-propargyne-NH2 hydrochloride is a thalidomide-derived ligand targeting the E3 ubiquitin ligase cereblon (CRBN). It facilitates the recruitment of CRBN for targeted protein degradation applications, making it instrumental in the development of PROTACs (proteolysis-targeting chimeras). This compound is valuable in cancer research and therapeutic studies focusing on protein regulation and degradation pathways.
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Thalidomide-PEG3-NH2 hydrochloride acts as a ligand for E3 ligase, specifically targeting the cereblon (CRBN) protein. This compound facilitates the recruitment of CRBN in protein degradation processes. It serves as a valuable tool for the development of Proteolysis Targeting Chimeras (PROTACs), enabling targeted protein degradation research in various biological studies.
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Thalidomide-NH-(CH2)3-NH-Boc is a Boc-modified thalidomide that serves as a ligand for cereblon (CRBN), facilitating the recruitment of CRBN protein within cellular systems. The Boc protecting group can be removed under acidic conditions, enabling its use in the synthesis of PROTAC (proteolysis-targeting chimeras) molecules. This compound plays a crucial role as an intermediate for synthesizing CRBN-based designed PROTACs, particularly those targeting 11β-substituted estradiol, making it valuable for research in targeted protein degradation and therapeutic development.
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Thalidomide-4-NH-PEG1-COO(t-Bu) functions as a ligand for E3 ligase, specifically targeting the Cereblon (CRBN) protein. This compound features a t-Bu protecting group, which can be cleaved under acidic conditions, enabling the synthesis of proteolysis-targeting chimeras (PROTACs). It serves as a crucial intermediate in the development of CRBN-based PROTAC molecules, facilitating targeted protein degradation for research applications in cancer and other diseases.
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AG6033 is a novel modulator of the cereblon (CRBN) protein. This compound effectively suppresses various tumor cell lines by influencing the interactions between CRBN and key antitumor target proteins, leading to the degradation of GSPT1 and IKZF1. AG6033 has demonstrated a CRBN-dependent cytotoxic effect, making it a valuable tool for research in cancer biology and the development of targeted therapies.
