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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.
PROTAC BRD4 ligand-2 is a specific ligand for the BRD4 protein, designed for use in PROTAC-mediated degradation strategies. This compound facilitates the targeted degradation of BRD4, a key regulator of transcription and associated with various cancers, by recruiting the E3 ubiquitin ligase. It is instrumental in research applications aimed at understanding BRD4's role in oncogenesis and therapeutic development in cancer treatments.
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SMARCA2/4-ligand-5 is a selective ligand targeting the SMARCA2 and SMARCA4 proteins, functioning as a crucial component in the PROTAC SMARCA2/4 degrader-37. This compound demonstrates potent biological activity, achieving an IC50 of ≤0.1 μM, making it suitable for applications in targeted protein degradation studies. Research utilizing SMARCA2/4-ligand-5 contributes to understanding the roles of these chromatin remodelers in various biological processes and cancer biology.
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BRAF ligand-1 acts as a specific ligand for the BRAF protein, playing a crucial role in the regulation of cell signaling pathways associated with cell proliferation, survival, and differentiation. This compound is important for studying the BRAF signaling pathway and its implications in various cancers. Additionally, BRAF ligand-1 can be utilized in the synthesis of CST905, further enhancing its utility in biochemical research and drug discovery efforts targeting mutant BRAF.
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LRRK2-IN-19 is a PROTAC target protein ligand designed for the synthesis of PROTAC JH-XII-03-02, a selective and potent LRRK2 degrader. This compound plays a crucial role in the modulation of LRRK2 activity, making it a valuable tool in Parkinson's disease research. Its ability to facilitate targeted protein degradation provides researchers with an innovative approach to investigating LRRK2-related pathways and potential therapeutic interventions.
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VHL Ligand 38 is a competitive inhibitor of the E3 ubiquitin-protein ligase VHL, exhibiting IC50 values of 4.1 μM and 7.0 μM in 1% and 10% DMSO, respectively. This compound features a hydroxyproline residue and an isoxazolylacetamide moiety, making it a valuable tool for research. VHL Ligand 38 effectively disrupts the interaction between VHL and a fluorescent peptide derived from HIF1α, facilitating studies on hypoxia-related signaling pathways and protein degradation mechanisms.
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TEAD Ligand 5 is a PROTAC ligand targeting TEAD proteins. It can be combined with an E3 ligase ligand and a linker to create PROTAC TEAD/IAP degrader-1, facilitating targeted protein degradation. This compound is instrumental in studies investigating TEAD-mediated signaling pathways and the development of novel therapeutic strategies.
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NSC682769 is a ligand specifically designed for the YAP protein, serving as a critical component in the development of PROTACs (proteolysis-targeting chimeras). This compound facilitates the targeted degradation of YAP, making it a valuable tool in research focused on cellular signaling pathways and oncogenesis. NSC682769 can be utilized in the synthesis of PROTAC YAP degrader-1, enabling the exploration of targeted protein degradation strategies in cancer biology.
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TEAD Ligand 1 is a specific ligand for the transcriptional enhancer factor TEAD. It serves as a crucial building block for the synthesis of PROTAC TEAD degrader-1, facilitating targeted degradation of TEAD proteins. This compound is essential for studies involving protein-protein interactions and the modulation of TEAD-related pathways in various biological research applications.
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DENV Ligand 1 is a selective ligand targeting the DENV envelope (E) protein, playing a crucial role in the development of PROTAC (Proteolysis Targeting Chimeras) reagents. It is essential for the synthesis of PROTAC Degrader ZXH-8-004, facilitating the targeted degradation of specific proteins within the cell. This compound has potential applications in studying viral pathogenesis and protein modulation.
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Mpro ligand 2 is a ligand specifically designed for the target protein involved in PROTAC applications. This compound plays a crucial role in the synthesis of PROTAC SARS-CoV-2 Mpro degrader-3, facilitating targeted protein degradation. Its ability to engage with the target protein makes it a valuable tool for research on SARS-CoV-2-related pathways and therapeutic strategies.
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POI ligand-2 is a specific ligand for the GPX4 protein, facilitating targeted protein degradation. This compound is instrumental in the synthesis of PROTACs, including PROTAC GPX4 degrader-5. Its application in protein research enables efficient modulation of GPX4 levels, aiding studies in mechanistic biology and therapeutic interventions targeting oxidative stress pathways.
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CDK8 Ligand 1 is a selective ligand for Cyclin-Dependent Kinase 8 (CDK8), a crucial regulator of transcriptional activity. This compound is instrumental in the development of proteolysis-targeting chimeras (PROTACs), enabling targeted degradation of protein substrates. Researchers can utilize CDK8 Ligand 1 to create customized molecular tools for studying CDK8-mediated signaling pathways and their implications in various diseases.
JH-VIII-49 is a potent and selective inhibitor of CDK8, exhibiting an IC50 value of 16 nM. Its unique steroid backbone design facilitates effective CDK8 inhibition, making it a valuable reagent for chemical research. JH-VIII-49 serves as a target protein ligand in the synthesis of PROTAC, specifically for the compound JH-XI-10-02, thereby advancing studies in targeted protein degradation and related therapeutic applications.
FN-1501-propionic acid is a ligand targeting cyclin-dependent kinases 2 and 9 (CDK2/9), utilized in the development of PROTAC (proteolysis targeting chimeras) for targeted protein degradation. This compound can be combined with a CRBN ligand to facilitate the design of PROTAC-based CDK2/9 degraders, enabling selective degradation of these kinases. Its application in research enhances the study of cellular processes regulated by CDK2 and CDK9, making it a valuable tool for investigating therapeutic strategies against diseases associated with dysregulated kinase activity.
CDK2/4 Ligand 1 is a specific ligand targeting cyclin-dependent kinases CDK2 and CDK4, designed for use in the development of proteolysis-targeting chimeras (PROTACs). It facilitates the synthesis of PROTAC CDK2/4 Degrader-1, enabling targeted degradation of these kinases to explore their role in various biological processes and cancers. This compound is essential for research applications focused on targeted protein degradation mechanisms.
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Palbociclib-C4-Boc is a Target Protein Ligand-Linker Conjugate that combines the CDK4/6 inhibitor Palbociclib with a PROTAC linker to facilitate E3 ligase recruitment. This compound is instrumental in synthesizing PROTAC BSJ-03-204, allowing for targeted protein degradation studies. It is particularly valuable in cancer research where modulation of cell cycle proteins is essential for therapeutic intervention.
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(R)-PROTAC CDK9 ligand-1 is a potent degrader targeting cyclin-dependent kinase 9 (CDK9), a key regulator of transcription and cell cycle progression. This compound facilitates the synthesis of PROTACs (proteolysis-targeting chimeras), which exhibit antitumor activity by promoting the degradation of CDK9. Research applications include investigations into cancer biology and therapeutic strategies aimed at modulating CDK9 levels for improved treatment outcomes.
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dTAG Targeting Ligand 1 is a ligand specifically designed for the targeted degradation of proteins using PROTAC technology. This compound facilitates the selective recruitment of E3 ligases to the target protein, promoting its ubiquitination and subsequent proteasomal degradation. dTAG Targeting Ligand 1 serves as a crucial tool in studies aimed at exploring protein function, validating drug targets, and developing novel therapeutic strategies through protein degradation.
SMARCA-BD ligand 1 for PROTAC hydrochloride is a selective ligand that specifically targets the BAF ATPase subunit SMARCA2. This compound facilitates the degradation of SMARCA2 through the PROTAC mechanism, making it a valuable tool for research into protein degradation pathways and epigenetic regulation. Its applications extend to studies on cancer biology and the development of targeted therapeutic strategies.
SMARCA-BD ligand 1 for PROTAC dihydrochloride is a selective ligand targeting the BAF ATPase subunit SMARCA2. This compound facilitates the proteolytic degradation of SMARCA2 through the PROTAC mechanism, thereby modulating its biological activity. It is utilized in research applications focused on the regulation of chromatin remodeling and exploring therapeutic avenues for diseases associated with altered SMARCA2 function.
SMARCA2 ligand-9 is a selective ligand for the target protein SMARCA2, designed for use in proteolysis-targeting chimera (PROTAC) applications. This compound facilitates the synthesis of PROTAC SMARCA2 degrader-27, enabling targeted degradation of SMARCA2 in cellular studies. Researchers can utilize SMARCA2 ligand-9 to investigate the role of SMARCA2 in various biological processes and assess its potential as a therapeutic target in cancer research and other diseases.
SMARCA2 ligand-13 is a targeted ligand designed for use in PROTAC (Proteolysis Targeting Chimera) applications, specifically interacting with the SMARCA2 protein. This compound facilitates the synthesis of PROTACs, enabling the targeted degradation of proteins associated with various diseases. Its primary utilization lies in the advancement of therapeutic strategies that leverage the ubiquitin-proteasome system for selective protein modulation in chemical biology research.
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SMARCA2 ligand-11 is a specific ligand for the chromatin remodeling factor SMARCA2, facilitating the development of PROTACs such as SMARCA2 degrader-32. This compound is instrumental in research applications focused on targeted protein degradation, particularly in studies aimed at elucidating the role of SMARCA2 in various biological processes and diseases. Its ability to selectively engage with SMARCA2 allows for investigations into novel therapeutic strategies in cancer and other conditions where SMARCA2 activity is implicated.
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SMARCA2 Ligand-Linker Conjugate-4 is designed as a targeted protein ligand-linker conjugate that includes a specific ligand for SMARCA2 along with a PROTAC linker to facilitate the recruitment of E3 ubiquitin ligases. This conjugate is instrumental in the synthesis of PROTAC SMARCA2 degrader-35, enabling the targeted degradation of SMARCA2 protein. Its applications extend to research in protein degradation mechanisms and the modulation of gene expression pathways involved in various diseases.
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Androgen Receptor Ligand 2 acts as a ligand for the androgen receptor, facilitating the targeted degradation of this protein through the PROTAC (proteolysis-targeting chimera) mechanism. This compound is integral for the synthesis of the PROTAC Androgen Receptor Degrader-1, enabling researchers to probe the functional role of the androgen receptor in various biological contexts. Its application extends to studies in cancer research and hormone-related disorders, where modulation of androgen receptor activity may serve as a therapeutic strategy.
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