PROTAC

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  1. Ligands for E3 Ligase

    3-(4-Hydroxy-1-oxoisoindolin-2-yl)piperidine-2,6-dione is a ligand for the E3 ligase cereblon (CRBN). This compound enables the targeted recruitment of CRBN, facilitating the degradation of specific proteins through the formation of proteolysis-targeting chimeras (PROTACs). It is a valuable tool for studying protein homeostasis and exploring therapeutic strategies in various diseases, including cancer.
  2. Ligands for E3 Ligase

    KB02-COOH is a chemical compound that serves as a ligand for E3 ligase, playing a crucial role in the ubiquitin-proteasome system. This fragment is essential for the synthesis of proteolysis-targeting chimeras (PROTACs), including variants such as KB02-JQ1 and KB02-SLF. Researchers can utilize KB02-COOH in studies focused on targeted protein degradation and the modulation of protein activity within cellular pathways.
  3. Ligands for E3 Ligase

    (S,R,S)-AHPC-Me dihydrochloride targets the von Hippel-Lindau (VHL) protein as a ligand for E3 ligase recruitment. This compound serves as a critical precursor for the synthesis of ARV-771, a PROTAC degrader that utilizes the VHL E3 ligase to facilitate the degradation of BET proteins. It has demonstrated potent activity in degrading BET proteins in castration-resistant prostate cancer (CRPC) cells, with a DC50 of less than 1 nM, highlighting its potential for therapeutic applications in cancer research.
  4. Lenalidomide Analog

    3-(6-Bromo-1-oxoisoindolin-2-yl)piperidine-2,6-dione functions as a Lenalidomide analog with potential utility in targeted protein degradation research. This compound exhibits properties that may facilitate the design of proteolysis-targeting chimeras (PROTACs), thereby enabling the selective degradation of proteins of interest. Further investigation into its biological activity could contribute to advancements in therapeutic strategies aimed at modulating cellular proteostasis and addressing various diseases.
  5. Ligands for E3 Ligase

    Lenalidomide-6-F is a modified derivative of Lenalidomide that functions as a ligand for the E3 ubiquitin ligase cereblon (CRBN). This compound effectively recruits CRBN, facilitating the targeted degradation of specific proteins via the PROTAC (proteolysis-targeting chimera) mechanism. Lenalidomide-6-F is valuable for research applications focused on the modulation of cellular protein levels and the development of novel therapeutic strategies in cancer and other diseases.
  6. CRBN Ligand

    2-Methoxyphenyl dihydrouracil serves as a ligand for the cereblon (CRBN) protein, enhancing its interaction in targeted protein degradation assays. This compound is valuable for the development of PROTACs (Proteolysis Targeting Chimeras), facilitating studies in targeted therapy and protein regulation. Its applications extend to research focused on modulating protein levels and understanding ubiquitin-proteasome system mechanisms.
  7. Mdm2 E3 Ligase Inhibitor

    MEL24 is an inhibitor of the Mdm2 E3 ligase, which plays a critical role in regulating p53 protein levels. This compound significantly reduces cell survival and enhances sensitivity to DNA-damaging agents in a p53-dependent manner. MEL24 is primarily utilized in antitumor research, contributing to studies aimed at understanding and overcoming resistance in cancer therapies.
  8. Ligands for E3 Ligase

    Lenalidomide 5'-piperazine-4-methylpiperidine hydrochloride is an E3 ligase ligand designed for PROTAC (proteolysis-targeting chimera) development. This compound serves as a protein degrader, featuring a terminal piperidine that facilitates further chemical modifications. Its unique structure allows for enhanced interaction with target proteins, making it a valuable tool for studying targeted protein degradation in various research applications.
  9. Thalidomide Analog

    Thalidomide acid is a Thalidomide analog that primarily functions as a target for Proteolysis Targeting Chimeras (PROTACs). It exhibits significant activity in modulating protein degradation and is utilized in chemical biology studies aimed at elucidating proteostasis and targeted therapeutics. This compound serves as a valuable tool in drug discovery and development, particularly for diseases related to dysregulated protein levels.
  10. Thalidomide Analog

    2-(2,6-Dioxopiperidin-3-yl)-5-ethynylisoindoline-1,3-dione is a Thalidomide analog primarily engaged in protein degradation pathways through PROTAC technology. Exhibiting modulatory effects on the immune system and anti-angiogenic properties, this compound is instrumental in investigational studies targeting multiple myeloma and other malignancies. Its distinctive structural attributes facilitate the exploration of targeted therapies and the development of innovative drug delivery platforms.
  11. Ligands for E3 Ligase

    3-(4-Bromo-2-chlorophenyl)piperidine-2,6-dione is a ligand for the CRBN-type E3 ubiquitin ligase, facilitating targeted protein degradation via the PROTAC (proteolysis-targeting chimeras) approach. This compound can be employed in the development of novel therapeutics that harness the ubiquitin-proteasome system for selective removal of specific proteins. Its applications are significant in disease models where modulation of protein levels is desired for research and therapeutic purposes.
  12. Thalidomide Analog

    2-(2,6-Dioxopiperidin-3-yl)-4-iodoisoindoline-1,3-dione is a Thalidomide analog that features an iodine substitution on the isoindoline structure. This compound exhibits significant biological activity related to anti-inflammatory and anti-angiogenic properties. It is primarily utilized in research applications investigating the mechanisms of action of Thalidomide and its derivatives in various therapeutic contexts, particularly in cancer and autoimmune disorders.
  13. Lenalidomide Derivative

    Lenalidomide-4-Br-7-fluoro is a derivative of Lenalidomide featuring bromine and fluorine substituents on the benzyl ring. This compound exhibits immunomodulatory properties, enhancing immune responses and exhibiting anti-tumor activity. It can be utilized in research to investigate the mechanisms of action of Lenalidomide and its analogs, as well as their potential therapeutic applications in hematological malignancies.
  14. Ligands for E3 Ligase

    1-(4-Pip-Ph)-DHP-dione is a ligand specifically designed for targeting E3 ligases. It plays a crucial role in the development of proteolysis-targeting chimeras (PROTACs), particularly in the synthesis of the HPK1 Degrader-2. This compound is valuable for research in targeted protein degradation and provides insights into E3 ligase-mediated cellular processes.
  15. CRBN Ligand

    N-Methylated pomalidomide acts as a selective ligand for cereblon (CRBN). This derivative of pomalidomide lacks the ability to recruit CRBN, making it a valuable negative control in studies involving pomalidomide. Additionally, N-methylated pomalidomide can be utilized in the synthesis of PROTACs, thereby assisting researchers in the exploration of targeted protein degradation pathways and mechanisms.
  16. Ligands for E3 Ligase

    VH032-OH is a ligand for the E3 ligase Von Hippel-Lindau (VHL), enabling targeted protein degradation. This compound can be utilized in the development of PROTACs (Proteolysis Targeting Chimeras) by linking it to target proteins. VH032-OH facilitates the selective ubiquitination and subsequent proteasomal degradation of substrate proteins, making it a valuable tool for investigating protein turnover and cellular regulation in various research applications.
  17. Lenalidomide Analog

    3-(7-Amino-1-oxoisoindolin-2-yl)piperidine-2,6-dione is a Lenalidomide analog that serves as a valuable tool in PROTAC research. This compound selectively modulates protein degradation pathways, making it instrumental in the development of targeted therapeutics. Its structural similarity to Lenalidomide allows for the exploration of novel therapeutic applications in oncology and immunology.
  18. Lenalidomide Analog

    3-(7-Bromo-1-oxoisoindolin-2-yl)piperidine-2,6-dione is a Lenalidomide analog targeting the ubiquitin-proteasome system. This compound exhibits notable biological activity in the development of PROTACs (proteolysis-targeting chimeras), providing a valuable tool for research into targeted protein degradation. Its structural features enhance the potential for therapeutic applications in oncology and related fields.
  19. Thalidomide Analogue

    Thalidomide-CH2NH2 hydrochloride is a Thalidomide analogue characterized by a primary amine functionality. This compound demonstrates potential biological activity by modulating immune responses and influencing angiogenesis. It is suitable for research applications investigating mechanisms of action related to inflammatory diseases, cancer treatment, and teratogenic effects associated with Thalidomide derivatives.
  20. Ligands for E3 Ligase

    Thalidomide-pyrrolidine is a ligand for E3 ligases, facilitating targeted protein degradation via the PROTAC technology. This compound is instrumental in the synthesis of PROTAC ARD-1676, which enables selective modulation of protein levels in cellular systems. Thalidomide-pyrrolidine is valuable for research applications focused on therapeutic interventions in various diseases by leveraging the ubiquitin-proteasome pathway.
  21. Ligands for E3 Ligase

    3-(4-Bromo-2-fluorophenyl)piperidine-2,6-dione is an effective ligand for the CRBN-type E3 ubiquitin ligase, facilitating targeted protein degradation through the formation of PROTACs (Proteolysis Targeting Chimeras). This compound is instrumental in studies focused on ubiquitin-mediated proteolysis and can be utilized in various research applications aimed at elucidating protein function and regulation. Its unique structural features enable specific binding interactions that are crucial for the development of innovative therapeutic strategies.
  22. Ligands for E3 Ligase

    E3 Ligase Ligand 18 is a selective ligand for E3 ubiquitin ligases, facilitating the targeted degradation of proteins through the ubiquitin-proteasome system. When conjugated to a target protein via a linker, it forms a PROTAC (proteolysis-targeting chimera), which effectively induces ubiquitination and subsequent degradation of cancer-associated proteins. This reagent is valuable in research focused on protein degradation pathways and may contribute to therapeutic strategies for cancer treatment.
  23. Ligands for E3 Ligase

    Cereblon inhibitor 1 is an isoindoline derivative that functions as a modulator of cereblon E3 ubiquitin ligase. This compound is designed to inhibit cerablon activity, making it a valuable tool for cancer research by disrupting protein homeostasis and influencing cell signaling pathways. Its application may extend to studying the therapeutic potential of targeting E3 ligases in various cancer models.
  24. Ligands for E3 Ligase

    Lenalidomide-4-aminomethyl hydrochloride is a derivative of Lenalidomide that functions as a ligand for cereblon (CRBN), a component of the E3 ubiquitin ligase complex. This compound facilitates the recruitment of CRBN protein, enabling targeted protein degradation. It can be utilized as a building block in the development of proteolysis-targeting chimeras (PROTACs) for various therapeutic applications in cancer research and other disease models.
  25. CRBN Ligand

    CRBN ligand-9 is a selective ligand targeting cereblon (CRBN) with a binding affinity (Ki) of 8.9 μM. This compound is designed for use in the synthesis of PROTACs (proteolysis targeting chimeras), facilitating the targeted degradation of specific proteins. CRBN ligand-9 serves as an essential tool for research in drug discovery and development, particularly in studies focused on targeted protein degradation mechanisms.
  26. CRBN Ligand

    CRBN ligand-187 is a potent CRBN-type E3 ubiquitin ligase ligand that plays a crucial role in the modulation of ubiquitination processes. This compound has been utilized for the synthesis of TQ-3959, facilitating research in targeted protein degradation and cellular signaling pathways. Its ability to engage the CRBN ligase offers valuable insights for studies involving protein homeostasis and therapeutic interventions in various diseases.
  27. Thalidomide Analog

    Thalidomide-1-Me-5-NH2 is an aminated analog of Thalidomide, primarily targeting E3 ligase activation. This compound serves as a useful intermediate for the development of PROTAC (Proteolysis Targeting Chimera) molecules through amine derivatization. Researchers can utilize this reagent in studies focused on targeted protein degradation and related therapeutic applications.
  28. Thalidomide Analog

    Deoxy-thalidomide-5-iodine is a Thalidomide analog that serves as a valuable tool in PROTAC (Proteolysis Targeting Chimeras) research. This compound is designed to facilitate targeted protein degradation by recruiting E3 ligases, enabling the selective elimination of specific proteins within cellular systems. Its unique structural modifications may enhance potency and efficacy in various biological assays, making it essential for advancing studies in targeted oncology and therapeutic interventions.
  29. Thalidomide Analog

    Thalidomide-4-carbaldehyde is a Thalidomide analogue featuring an aldehyde functional group. This compound is known to recruit E3 ligases, facilitating the ubiquitination and subsequent proteolysis of target proteins, making it a valuable tool in studying protein degradation pathways. Its highly reactive aldehyde group engages in reductive amination reactions with amine nucleophiles, offering diverse applications in chemical biology and medicinal chemistry research.
  30. Thalidomide Analog

    Thalidomide-5-carbaldehyde is a Thalidomide analog featuring an aldehyde functional group. It actively interacts with E3 ligases, facilitating the ubiquitination and degradation of specific target proteins, thereby contributing to cellular regulation. The aldehyde group exhibits high reactivity towards amine nucleophiles, enabling reductive amination and other chemical modifications, making it a valuable tool for research in protein degradation pathways and therapeutic development.
  31. Thalidomide Analog

    Thalidomide-1-Me,4-OH is an analogue of Thalidomide, featuring an additional methyl group on the glutarimide moiety. This modification abolishes its interaction with the E3 ubiquitin ligase, cereblon (CRBN), which is critical for the ubiquitination and subsequent proteolytic degradation of target proteins. Thalidomide itself is well-known for its immunomodulatory and anti-inflammatory properties, making Thalidomide-1-Me,4-OH a valuable tool for investigating the molecular mechanisms of CRBN-mediated drug action and cellular protein regulation in research applications.
  32. Ligands for E3 Ligase

    CRBN ligand-47 is a potent ligand for the CRBN-type E3 ubiquitin ligase, facilitating targeted protein degradation through the formation of PROTACs (Proteolysis Targeting Chimeras). This compound exhibits effective recruitment of E3 ligase activity, making it valuable for research in protein homeostasis and therapeutic interventions in various diseases. Its role in modulating ubiquitin-mediated pathways underscores its utility in chemical biology and drug discovery applications.
  33. Immunomodulatory/Antineoplastic Agent

    Lenalidomide hydrochloride is an oral immunomodulatory agent targeting cereblon (CRBN), acting as a molecular glue. It promotes the selective ubiquitination and degradation of transcription factors IKZF1 and IKZF3 via the CRBN-CRL4 ubiquitin ligase complex. This mechanism effectively inhibits the growth of mature B-cell lymphomas, including multiple myeloma, while also inducing the release of IL-2 from T cells, making it valuable in cancer research and therapeutic applications.
  34. Ligands for E3 Ligase

    Lenalidomide-5-aminomethyl is a cereblon (CRBN) ligand that facilitates the recruitment of the CRBN protein, enabling targeted cellular degradation. This compound can be utilized as a key component in the development of PROTACs (proteolysis-targeting chimeras), which harness the ubiquitin-proteasome system for the selective degradation of specific proteins. Its significant role in E3 ligase-mediated pathways makes it valuable for research in targeted protein modulation and therapeutic development.
  35. E3 Ligase Ligand

    E3 Ligase Ligand 26 is a selective ligand for E3 ubiquitin ligases, facilitating the development of proteolysis-targeting chimeras (PROTACs). This compound plays a crucial role in the synthesis of the PROTAC SOS1 degrader, contributing to targeted protein degradation research. Its application extends to studies of cellular pathways and potential therapeutic interventions for various diseases through the modulation of protein levels.
  36. Ligands for E3 Ligase

    E3 ligase Ligand 42 is an E3 ubiquitin ligase ligand designed for targeted protein degradation applications. It can be conjugated to a target protein ligand via a linker, facilitating the synthesis of PROTAC AR Degrader-6. This compound effectively induces ubiquitination and subsequent degradation of proteins associated with cancer progression, making it a valuable tool for research in cancer biology and therapeutic development.
  37. Ligands for E3 Ligase

    (R,S,S)-VH032-Me is a ligand for E3 ubiquitin ligase, playing a crucial role in targeted protein degradation through the ubiquitin-proteasome pathway. It can be conjugated to proteins via a linker to create PROTACs such as dTAGV-1-NEG, which facilitate the selective degradation of oncogenic proteins. This compound is essential for studies involving targeted protein degradation, offering valuable insights into cancer biology and therapeutic development.

  38. Ligands for E3 Ligase

    KLHDC2-IN-1 is a ligand that specifically targets the ubiquitin E3 ligase KLHDC2, exhibiting a dissociation constant (Kd) of 160 nM. This compound facilitates the development of PROTACs, which are designed to induce degradation of BRD4 in cellular environments. Its application in cellular research underscores its potential utility in studying protein degradation mechanisms and therapeutic strategies targeting BRD4-related pathways.
  39. Ligands for E3 Ligase

    E3 ligase Ligand 58 is a selective ligand for E3 ligases, facilitating the synthesis of proteolysis-targeting chimeras (PROTACs). This compound plays a critical role in targeted protein degradation, enabling researchers to explore cellular mechanisms and therapeutic applications. E3 ligase Ligand 58 serves as a valuable tool in drug development and biological research focused on post-translational modifications.
  40. Ligands for E3 Ligase

    CRBN ligand-17 is an E3 ubiquitin ligase ligand that targets the cereblon (CRBN) substrate recognition domain. This compound is essential for the design and synthesis of PROTACs (proteolysis-targeting chimeras), which facilitate targeted protein degradation. Its application in research includes studying protein regulation mechanisms and investigating therapeutic strategies for various diseases.
  41. Ligands for E3 Ligase

    Deoxy-thalidomide-OMe is an E3 ligase ligand that plays a crucial role in targeted protein degradation mechanisms. This compound is utilized in the synthesis of PROTAC LRRK2 Degrader-4, facilitating research in the modulation of LRRK2 activity, which has implications in neurodegenerative diseases. Its ability to selectively engage with E3 ligases makes it a valuable tool for advancing studies in protein homeostasis and therapeutic development.
  42. Ligands for E3 Ligase

    RA183 is a selective ligand for E3 ligases, facilitating the development of proteolysis-targeting chimeras (PROTACs). This compound enables the targeted degradation of specific proteins by harnessing the ubiquitin-proteasome system, making it a valuable tool in chemical biology and drug discovery. RA183 can be utilized in various research applications aimed at elucidating protein function and developing innovative therapeutic strategies.
  43. Ligands for E3 Ligase

    Lenalidomide-4-aminomethyl is an E3 ligase ligand that specifically targets cereblon (CRBN), facilitating the recruitment of CRBN protein. This compound serves as an essential building block for the development of PROTAC molecules, enabling targeted protein degradation research. Its unique structural features make it a valuable tool for studying CRBN-mediated pathways and exploring therapeutic applications in cancer and other diseases.
  44. Ligands for E3 Ligase

    Cyclopropane-(S,R,S)-AHPC is a selective ligand for E3 ubiquitin ligases, which play a crucial role in ubiquitination processes affecting protein degradation and cellular regulation. This compound is valuable for research into post-translational modifications and protein interactions, enabling studies into cellular signaling pathways and disease mechanisms. Its ability to modulate E3 ligase activity makes it an essential tool for understanding protein homeostasis and developing targeted therapies.
  45. Ligands for E3 Ligase

    E3 Ligase Ligand 44 serves as an effective ligand for E3 ligases, facilitating the development of proteolysis-targeting chimeras (PROTACs) such as the AR Degrader-7. Its primary mechanism involves engaging E3 ligases to promote targeted protein degradation, enabling precise modulation of cellular pathways. This compound is useful in research focused on protein homeostasis, targeted therapy, and the exploration of novel therapeutic strategies in cancer and other diseases.
  46. Ligands for E3 Ligase

    VH032 analogue-2 is a selective ligand for the E3 ubiquitin ligase von Hippel-Lindau (VHL), facilitating its recruitment in cellular processes. This compound effectively removes its protective group under acidic conditions, enabling its direct utilization in the synthesis of PROTAC (Proteolysis Targeting Chimeras) molecules. VH032 analogue-2 serves as a crucial intermediate for the development of VHL-based PROTACs, making it a valuable tool for research in targeted protein degradation and related fields.
  47. E3 Ligase Ligand

    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.
  48. Ligands for E3 Ligase

    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.
  49. Ligands for E3 Ligase

    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.
  50. Ligands for E3 Ligase Chemical

    (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.

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