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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,S,S)-VH032 is a ligand for the E3 ubiquitin ligase von Hippel-Lindau (VHL), enabling targeted protein degradation through the formation of PROTACs. It plays a crucial role in the synthesis of PROTAC SGK3 degrader-2, facilitating the selective degradation of SGK3 and other target proteins. This compound is valuable for research in protein regulation and targeted therapeutic strategies.
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E3 Ligase Ligand 25 is a selective ligand for the E3 ubiquitin ligase, facilitating the synthesis of PROTACs, specifically the SOS1 degrader. This compound serves as a critical tool in studies aimed at targeted protein degradation, contributing to the advancement of therapeutic strategies in cancer and other diseases. Researchers can leverage E3 Ligase Ligand 25 to explore ubiquitin-mediated proteolysis and its implications in cellular regulation.
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Acepromazine-OTs is a ligand for the E3 ligase TRIM21, facilitating the recruitment of this protein in cellular contexts. It can be conjugated to target proteins via a linker to create PROTAC molecules, such as TrimTAC1. Acepromazine-OTs is valuable in research for deciphering protein degradation pathways and exploring targeted protein modulation approaches in therapeutic applications.
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E3 ligase Ligand 21 is a potent cereblon binder that facilitates the targeted degradation of Ikaros and Aiolos via the ubiquitin-proteasome pathway. This compound is valuable for research applications focusing on the modulation of transcription factors involved in hematologic malignancies and immune regulation. Its ability to selectively promote protein degradation makes it an important tool in the study of cellular homeostasis and targeted therapy development.
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E3 ligase Ligand 60 is a selective ligand for E3 ligase, facilitating the synthesis of JV8. This compound plays a pivotal role in targeted protein degradation research and investigation of E3 ligase-mediated pathways. It holds potential for advancing therapeutic strategies in various diseases by modulating protein levels through ubiquitin-proteasome pathways.
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Lenalidomide 5'-piperazine is an E3 ligase ligand that functions as a Cereblon (CRBN) recruitor. This compound can be utilized to create PROTAC (Proteolysis Targeting Chimeras) molecules by linking it to various target protein ligands through a suitable linker. Research applications include the study of targeted protein degradation and the modulation of cellular pathways related to tumorigenesis.
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VH032-CH2-Boc is a Boc-modified variant of VH032 that functions as a ligand for the E3 ubiquitin ligase von Hippel-Lindau (VHL) protein. This compound is designed to remove the protecting group under acidic conditions, making it suitable for direct incorporation into the synthesis of PROTAC molecules. VH032-CH2-Boc serves as a critical intermediate in the development of PROTACs targeting VHL, facilitating the targeted degradation of various proteins for research applications in drug discovery and cellular biology.
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SJ46411 is a potent ligand for KLHDC2, demonstrating a binding affinity with a Kd of approximately 260 nM as determined by isothermal titration calorimetry. Additional characterization includes SPR Kd of 0.5 μM and a TR-FRET IC50 of 3.9 μM, alongside a notable increase in thermal stability indicated by a ΔTm of 6.0 °C. This compound is valuable for research involving KLHDC2 interactions and can aid in elucidating its biological roles and potential as a therapeutic target.
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(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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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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