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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.
(S)-Deoxy-thalidomide functions as a ligand for E3 ubiquitin ligases, facilitating targeted protein degradation. When conjugated to a target protein via a linker, it forms PROTAC K-Ras Degrader-3, which specifically degrades KRAS mutant proteins. This compound is valuable for research applications in cancer therapeutics, particularly in studies aiming to modulate pathways involving KRAS mutations.
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E3 Ligase Ligand 13 functions as a ligand for E3 ubiquitin ligases, facilitating the creation of PROTACs (proteolysis-targeting chimeras). These PROTACs are designed to induce ubiquitination-mediated degradation of proteins associated with cancer progression. This compound is essential for research focused on targeted protein degradation and the development of novel therapeutic strategies in oncology.
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(R)-Pomalidomide-pyrrolidine is a ligand for the E3 ubiquitin ligase CRBN. It facilitates targeted protein degradation and is instrumental in the development of PROTACs (proteolysis-targeting chimeras). This compound is employed in research to explore novel therapeutic strategies for diverse diseases by harnessing the ubiquitin-proteasome system.
(S,R,S,R)-AHPC-Me is a ligand for the von Hippel-Lindau (VHL) protein, promoting its recruitment in cellular processes. This compound is valuable for research applications involving the regulation of hypoxia-inducible factors (HIFs) and the study of oxygen sensing pathways. Its unique properties enable researchers to explore the mechanisms of VHL-mediated ubiquitination and degradation of target proteins, contributing to a better understanding of various cancers and metabolic disorders.
Thalidomide-azetidine-CHO is a synthesized ligand designed for E3 ligase applications, incorporating the thalidomide-based cereblon ligand. This compound enables targeted protein degradation through the PROTAC technology, facilitating precise modulation of protein levels within cells. Its key biological activity and role as a linker conjugate make it suitable for diverse research applications in drug discovery and cellular biology.
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VH032 analogue-1 is an E3 ligase ligand that targets the von Hippel-Lindau (VHL) protein, facilitating its recruitment. This analogue serves as a key intermediate in the synthesis of PROTAC molecules by removing protective groups under acidic conditions. Its role in PROTAC synthesis makes it a valuable tool for researchers developing targeted protein degradation strategies.
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(R,S,S)-VH032-Me TFA is a selective E3 ligase ligand that serves as a crucial tool for the development of targeted protein degradation strategies. This compound is utilized in the synthesis of dTAGV-1 hydrochloride, facilitating research into ubiquitin-proteasome system modulation and its implications in cancer and cellular biology. Its ability to modulate E3 ligase activity makes it valuable for investigating innovative therapeutic approaches in biomedical research.
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BCL-xL/BCL-2 Ligand 1 is a selective ligand targeting BCL-xL and BCL-2 proteins. This compound serves as a crucial component in the development of PROTACs (proteolysis-targeting chimeras), which promote targeted degradation of specific proteins through E3 ligase recruitment. It is valuable for research focused on apoptosis, cancer biology, and therapeutic development aimed at modulating cell survival pathways.
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(3S)Lenalidomide-5-Br is a potent ligand for E3 ubiquitin ligases, facilitating targeted protein degradation through the ubiquitin-proteasome system. This compound is instrumental in research applications involving the development of PROTACs, notably in the synthesis of Cbl-b-IN-1. Its unique structure allows for specific interaction with target proteins, making it a valuable tool in cellular and molecular biology studies.
VH032-NH-CO-CH2-NHBoc is a Boc-modified ligand that targets the von Hippel-Lindau (VHL) protein, functioning as a crucial component for developing Proteolysis Targeting Chimeras (PROTACs). This compound facilitates the recruitment of VHL to specific target proteins, enabling targeted degradation of these proteins through the ubiquitin-proteasome pathway. Under acidic conditions, VH032-NH-CO-CH2-NHBoc removes the Boc protection, allowing for the formation of PROTAC molecules that capitalize on VHL's E3 ligase activity. Its application is significant in studies focusing on targeted protein degradation and therapeutic development.
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CRBN Ligand-191 is an E3 ligase ligand that targets the cereblon (CRBN) protein, facilitating ubiquitination and subsequent degradation of tagged substrates. This compound is essential in the synthesis of PROTACs, such as the PROTAC ALK degrader-4, which enables selective degradation of specific oncoproteins. Researchers can utilize CRBN Ligand-191 to explore targeted protein degradation mechanisms and study protein homeostasis in various biological contexts.
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VHL Ligand 36 is a selective ligand for the von Hippel-Lindau (VHL) E3 ligase, facilitating targeted ubiquitination of substrate proteins. This compound is instrumental in research applications focused on studying the VHL pathway and its implications in various cellular processes, including tumorigenesis and hypoxia response. Additionally, VHL Ligand 36 serves as a precursor for synthesizing SD-2301, expanding its utility in chemical biology investigations.
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All 3 sizes![4-[(1E)-2-Nitroethenyl]benzoic acid](https://www.adooq.com/media/catalog/product/cache/16359f9c8ddfa823fcb5503b1e11b7ae/a/8/a80640-4-1e-2-nitroethenyl-benzoic-acid.gif)
4-[(1E)-2-Nitroethenyl]benzoic acid is a specific ligand for E3 ligase, which plays a crucial role in ubiquitination and protein degradation. This compound facilitates the synthesis of PROTAC BRD4 Degrader-38, enabling targeted degradation of specific proteins within cellular pathways. Its application in protein targeting and degradation makes it a valuable tool for researchers investigating proteostasis and related therapeutic interventions.
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E3 Ligase Ligand 54 is a selective ligand for the E3 ubiquitin ligase Cereblon, playing a crucial role in targeted protein degradation. This compound facilitates the synthesis of PROTAC Degrader SJ44236, enabling the investigation of protein homeostasis and therapeutic strategies in cancer research. Its utility in studying ubiquitin-proteasome pathways makes it a valuable tool for drug discovery and development.
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Pomalidomide 5'-fluoro-6'-piperazine-4-methylpiperidine hydrochloride is a ligand that targets the E3 ubiquitin ligase cereblon (CRBN). This compound is designed to facilitate the recruitment of cereblon protein for targeted protein degradation. Pomalidomide 5'-fluoro-6'-piperazine-4-methylpiperidine hydrochloride can be utilized in the development of PROTACs by linking to other protein ligands, enabling innovative research in protein homeostasis and disease modulation.
DCAF11 ligand 2 is an E3 ligase ligand that facilitates the recruitment of DCAF11. This compound is essential for the development of PROTACs, specifically for synthesizing the BRD4 degrader LGF308, which targets BRD4 for ubiquitination and proteasomal degradation. The ability to harness DCAF11 ligand 2 in research applications contributes significantly to the advancement of targeted protein degradation strategies.
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CRBN ligand-895 is an E3 ubiquitin ligase ligand that specifically targets cereblon (CRBN), facilitating the recruitment of this crucial protein. This compound serves as a valuable building block for the synthesis of PROTACs, including PROTAC HDAC8 Degrader-4. Its application extends to the study of protein degradation pathways and the development of innovative therapeutic strategies in various disease models.
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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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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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