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Ligands for target proteins in PROTAC design bind the protein that a degrader is meant to remove. A proteolysis-targeting chimera (PROTAC) joins such a ligand to an E3 ubiquitin ligase ligand through a linker, so that the ligase ubiquitinates the bound target. Most entries are known inhibitors or receptor ligands modified with an attachment point, such as an aldehyde, amine, carboxylic acid or alkyne group. Dasatinib carbaldehyde and Imatinib carbaldehyde are aldehyde-bearing analogs of two kinase inhibitors. BI-4464 binds protein tyrosine kinase 2 (PTK2), also called focal adhesion kinase (FAK), and SirReal1-O-propargyl carries a propargyl handle on a sirtuin 2 (SIRT2) ligand. Receptor ligands in the list include Estrone-N-O-C1-amido and AP1867-2-(carboxymethoxy), which binds FK506-binding proteins.
IBT6A-CO-ethyne is a ligand specifically designed for the target protein in PROTAC applications. This compound facilitates the synthesis of IBT6A, enabling studies in targeted protein degradation. Its use in protein-protein interaction assays can enhance understanding of the underlying molecular mechanisms in cellular processes.
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Napabucasin analogue is a ligand for target proteins utilized in PROTAC (Proteolysis Targeting Chimeras) development. This compound facilitates selective degradation of target proteins, providing a powerful tool for studying protein function and therapeutic interventions. Additionally, it can be employed in the synthesis of Napabucasin, enhancing approaches in cancer research and other biomedical applications.
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PXR Ligand 3 is a ligand for the Pregnane X Receptor (PXR), acting as a critical component in the development of PROTAC (Proteolysis Targeting Chimera) molecules. It facilitates the recruitment of E3 ubiquitin ligases, thereby promoting targeted degradation of specific proteins. This compound is valuable in drug discovery and biochemical research, particularly in studies focused on the modulation of PXR activity and the development of PROTAC-based therapeutics.
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IRAK4 ligand-12 is a ligand for interleukin-1 receptor-associated kinase 4 (IRAK4), designed for use in PROTAC (proteolysis targeting chimeras) applications. This compound plays a critical role in the selective degradation of IRAK4, thus enabling the modulation of immune response pathways. It is particularly useful in research focused on inflammation and cancer, facilitating studies on targeted protein degradation strategies. IRAK4 ligand-12 can also be utilized in the synthesis of KTX-951, contributing to advancements in therapeutic development.
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SHP2 ligand-3 is a ligand specifically designed for the SHP2 target protein, facilitating the synthesis of SHP2 protein degrader-1. This compound serves as an essential tool in targeted protein degradation studies, enabling the selective degradation of SHP2. Its application in PROTAC technology allows researchers to investigate the functional roles of SHP2 in cellular processes and disease mechanisms, supporting drug discovery and development efforts.
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BCN-sulfonamide-PEG2-sulfonamide-N-bis(ethanol) serves as a versatile ligand for target proteins in PROTAC applications. This compound incorporates a sulfonamide linker designed to enhance the solubility of linker-conjugates. It is particularly useful in the synthesis of PROTACs aimed at inducing targeted degradation of proteins with potential antitumor activity.
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AZD9496 deacrylic acid phenol is a ligand targeting specific protein associated with PROTAC (Proteolysis Targeting Chimeras) technology. This compound plays a critical role in the design of selective ER (estrogen receptor) degraders, facilitating targeted protein degradation. Its use in research applications allows for the exploration of novel therapeutic strategies in cancer and other estrogen-related diseases.
SMARCA2/4-ligand-6 is a small molecule ligand specific for the SMARCA2 and SMARCA4 proteins, facilitating targeted protein degradation via the PROTAC (Proteolysis Targeting Chimeras) technology. This compound can be utilized in the development of PROTACs aimed at studying the roles of these epigenetic regulators in cancer biology and other diseases. SMARCA2/4-ligand-6 is a valuable tool for researchers investigating targeted therapeutic strategies and protein homeostasis.
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CSI118 TFA is a ligand for targeted protein degradation utilizing the PROTAC (Proteolysis Targeting Chimera) strategy. This compound has demonstrated the ability to effectively engage target proteins, facilitating their ubiquitination and subsequent proteasomal degradation. It serves as a valuable tool for researchers investigating targeted protein degradation mechanisms and developing novel therapeutic strategies. Additionally, CSI118 TFA can be utilized in the synthesis of CSI86, expanding its application in chemical biology research.
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FLT3 ligand-2 is a potent ligand for the FLT3 target protein, facilitating the development of PROTACs (proteolysis-targeting chimeras). This compound is utilized to synthesize PROTAC FLT-3 degrader 1, which promotes the selective degradation of FLT3 in targeted therapies. Its application is crucial in research focused on eradicating FLT3-driven malignancies, contributing to advancements in cancer treatment strategies.
BTK-IN-39 is a ligand targeting Bruton’s tyrosine kinase (BTK), designed for the synthesis of PROTAC BTK Degrader-11. This compound enables the selective degradation of BTK, facilitating studies on its biological functions and role in disease models, particularly in hematological malignancies. Its application in PROTAC technology allows for innovative approaches to therapeutic intervention by modulating protein levels within cells.
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Synonyms: PROTAC ABL binding moiety 3
HG-7-85-01-Decyclopropane is a ligand for target proteins utilized in the PROTAC (Proteolysis Targeting Chimera) technology. This compound features the ABL inhibitor moiety and binds to IAP (inhibitor of apoptosis protein) ligands through a linker, enabling the targeted degradation of specific proteins within cells. Its application in research includes elucidating protein function and pathway regulation, making it a valuable tool in cancer biology and therapeutic development.
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Cbl-b-IN-21 is a ligand specifically designed for the Cbl-b target protein, facilitating the development of PROTAC-based therapeutic strategies. This compound enhances the targeted degradation of Cbl-b, making it valuable in research applications focused on modulating ubiquitin-mediated protein turnover. Cbl-b-IN-21 is instrumental in synthesizing the PROTAC Cbl-b-IN-1, enabling studies on targeted protein degradation pathways.
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SMI-1074 is a ligand for target proteins in the development of PROTACs (Proteolysis Targeting Chimeras). It facilitates the targeted degradation of specific proteins, making it a valuable tool in research areas such as cancer biology and cellular regulation. SMI-1074 is also instrumental in the synthesis of related compounds SMD-3236 and SMD-1087, expanding its utility in chemical biology studies.
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mTOR ligand 1 is a potent ligand targeting the mechanistic target of rapamycin (mTOR) for use in PROTAC (Proteolysis Targeting Chimera) applications. This compound plays a crucial role in the degradation of mTOR through the ubiquitin-proteasome system, enabling selective modulation of mTOR activity. mTOR ligand 1 is ideal for research involving mTOR signaling pathways and related cellular processes, providing a valuable tool for investigating therapeutic strategies in cancer and metabolic disorders.
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SMARCA2/4-ligand-4 acts as a ligand for the SMARCA2 and SMARCA4 proteins, serving as an essential component for the development of Proteolysis Targeting Chimeras (PROTACs). This compound facilitates the targeted degradation of proteins associated with various cellular processes, providing a powerful tool for drug discovery and therapeutic research. SMARCA2/4-ligand-4 is integral to the synthesis of PROTAC SMARCA2/4 degrader-36, enabling investigations into the modulation of oncogenic pathways and protein homeostasis.
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PROTAC BRD4 ligand-3 is a specialized ligand designed to engage the BRD4 protein for targeted protein degradation applications via the PROTAC (proteolysis-targeting chimeras) technology. This compound facilitates the synthesis of PROTAC BRD4 Degrader-27, providing a valuable tool for research in targeted therapeutics and the study of BRD4-related pathways in various diseases, including cancer. Its ability to promote the selective degradation of BRD4 makes it instrumental for investigating the functional role of this protein in cellular processes.
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Multi Kinase Ligand 4 is a selective ligand designed for the synthesis of PROTACs, specifically PROTAC DB-0646. This compound plays a crucial role in modulating protein degradation pathways, facilitating targeted protein degradation through the ubiquitin-proteasome system. Its applications extend to drug discovery and development in cancer research, enabling investigations into the regulation of kinase activity and potential therapeutic interventions.
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TBL1X ligand 1 is a target protein ligand designed for use in the synthesis of PROTAC TBL1X degrader-1. This compound facilitates the targeted degradation of proteins associated with various biological processes. Its application in research extends to studying the modulation of TBL1X-related pathways and advancing therapeutic strategies in disease contexts where protein degradation is of interest.
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SMARCA2 ligand-7 is a specific ligand for SMARCA2, a key protein involved in chromatin remodeling. This compound is designed for use in PROTAC (PROteolysis TArgeting Chimeras) studies, facilitating targeted protein degradation. SMARCA2 ligand-7 enables researchers to investigate the functional roles of SMARCA2 in cellular processes and its potential as a therapeutic target in various diseases.
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BTK Ligand 15 is a specific ligand for Bruton's tyrosine kinase (BTK) and serves as a crucial component in the development of PROTAC BTK Degrader-13. This compound enables the selective degradation of BTK, providing a powerful tool for investigating BTK's role in various diseases, particularly in B-cell malignancies. Researchers can leverage BTK Ligand 15 to elucidate BTK signaling pathways and explore therapeutic strategies targeting BTK-dependent conditions.
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BRD9 ligand-5 is a selective ligand targeting BRD9, designed for use in PROTAC (Proteolysis Targeting Chimeras) applications. This compound facilitates targeted degradation of specific proteins, enabling the study of protein function and therapeutic development. Additionally, BRD9 ligand-5 can be utilized in the synthesis of CFT8634, allowing researchers to explore its biological activities and potential therapeutic effects.
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Demethyl-RSL3-boc is a ligand designed for targeted protein degradation through PROTAC (Proteolysis Targeting Chimeras) technology. This compound effectively interacts with target proteins to facilitate their ubiquitin-mediated degradation, thereby modulating cellular pathways. Demethyl-RSL3-boc is utilized in research applications focused on studying protein dynamics and developing novel therapeutic strategies for various diseases, including cancer.
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SMARCA2/4-ligand-1 is a selective ligand for the proteins SMARCA2 and SMARCA4, facilitating targeted protein degradation via PROTAC (Proteolysis Targeting Chimeras) technology. This compound exhibits promising biological activity by promoting the ubquitination and subsequent degradation of these target proteins. It is designed for use in research applications focusing on gene regulation, chromatin remodeling, and the study of protein homeostasis.
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BRM/BRG1 ligand 3 is a target protein ligand designed for the synthesis of PROTAC BRM/BRG1 degrader-3. This compound facilitates the targeted degradation of BRM and BRG1 proteins, thereby modulating their biological activity. Its application is pivotal in studies focused on chromatin remodeling and cancer biology, enabling researchers to explore the therapeutic potential of targeted protein degradation.
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