PROTAC

Items 5501-5550 of 5610

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  1. PROTAC Linkers

    1,1,1-Trifluoroethyl-PEG4-aminooxy is a polyethylene glycol (PEG)-based linker designed for use in the synthesis of PROTAC (proteolysis-targeting chimeras). This compound facilitates the conjugation of ligands for targeted protein degradation, enabling selective modulation of protein levels in biological systems. Its unique structure supports efficient and stable interactions, making it suitable for research applications in drug development and cellular biology studies focused on degrading specific proteins.
  2. PROTAC Linkers

    m-PEG3-S-Acetyl is a PEG-derived linker designed for use in the synthesis of PROTACs (Proteolysis Targeting Chimeras). This compound facilitates the conjugation of the targeting ligand to the E3 ubiquitin ligase, enhancing the degradation of specific proteins within cells. Its application is crucial for researchers developing targeted protein degradation technologies to explore cellular mechanisms and therapeutic interventions.
  3. PROTAC Linkers

    TCO-PEG4-TCO is a PEG-based linker designed for use in PROTAC (Proteolysis Targeting Chimera) synthesis. This compound plays a crucial role in facilitating the targeted degradation of specific proteins, enabling the development of novel therapeutic strategies. Its application in research underscores its importance in the fields of protein modulation and targeted therapy.
  4. PROTAC Linkers

    m-PEG5-Boc is a PEG-based PROTAC linker that facilitates the synthesis of proteolysis-targeting chimeras (PROTACs). This compound effectively enhances the solubility and stability of the PROTAC molecule, promoting efficient protein degradation. It is particularly valuable in chemical biology research for the development of targeted protein degradation strategies.
  5. PROTAC Linkers

    Boc-NH-PEG20-CH2CH2COOH is a PEG-derived linker designed for use in the synthesis of proteolysis-targeting chimeras (PROTACs). This compound facilitates the recruitment of E3 ligases to specific target proteins, enabling targeted degradation pathways. Its unique chemical structure enhances solubility and stability, making it an essential tool for researchers investigating ubiquitin-proteasome system modulation and targeted protein degradation applications.
  6. PROTAC Linkers

    Iodoacetyl-PEG4-NHS ester is a PEG-based linker designed for the synthesis of PROTACs (proteolysis-targeting chimeras). This compound contains an iodoacetyl group that facilitates efficient conjugation to target proteins, enabling targeted degradation through the ubiquitin-proteasome system. Its versatility in forming stable linkages makes it valuable for researchers investigating targeted protein degradation and related therapeutic applications.
  7. PROTAC Linker

    Boc-aminooxy-PEG2-propargyl is a PEG-based linker designed for the synthesis of PROTACs (proteolysis-targeting chimeras). It features an alkyne functional group, enabling it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc) reactions with azide-containing molecules. This compound is essential for developing targeted protein degradation strategies and facilitates the construction of complex molecular architectures in chemical biology research.
  8. PROTAC Linker

    N-(Aminooxy-PEG3)-N-bis(PEG4-Boc) is a PEG-based linker designed for use in the synthesis of PROTACs (proteolysis-targeting chimeras). This compound facilitates the conjugation of a target protein to an E3 ligase, enabling targeted protein degradation. Its construction of aminooxy and Boc-protected entities allows for functionalization and versatility in drug design, making it a valuable tool for researchers exploring targeted therapies and protein modulation.
  9. PROTAC Linker

    Ethyl-PEG4-alcohol is a polyethylene glycol (PEG)-based linker utilized in the synthesis of PROTACs (Proteolysis Targeting Chimeras). This compound enhances solubility and facilitates the efficient conjugation of a target protein ligand with an E3 ligase ligand, enabling selective degradation of target proteins. It is primarily applied in chemical biology and drug discovery to investigate protein function and modulation.
  10. PROTAC

    ERK-CLIPTAC is a PROTAC molecule designed to selectively induce the degradation of extracellular signal-regulated kinase (ERK). By harnessing the cellular ubiquitin-proteasome system, it offers a novel approach to modulate ERK activity. This compound is valuable for research applications focused on ERK-related signaling pathways and their implications in various diseases, including cancer and neurodegenerative disorders.
  11. PHOTACs

    Photo-lenalidomide-acid is a photochemical agent designed for use in PHOTACs (photo-controllable PROTACs). This compound consists of an E3 ligase ligand linked to a photoswitch and a ligand specific to a protein of interest, allowing precise optical control of protein degradation. Its innovative mechanism facilitates targeted protein modulation in cellular studies and therapeutic applications, making it a valuable tool for researchers investigating protein dynamics.
  12. PROTAC VHL Degrader

    CMP98 is a PROTAC designed as a negative control for CM11, targeting the von Hippel-Lindau (VHL) protein. Unlike its active counterparts, CMP98 does not induce degradation of VHL, making it a valuable tool for validating the specificity and efficacy of VHL-dependent degradation studies. This compound can be utilized in research applications involving protein degradation pathways and the exploration of PROTAC mechanisms.
  13. ERα Y537S Degrader

    PROTAC ERα Y537S degrader-1 is designed to selectively target and degrade the estrogen receptor-alpha (ERα) variant Y537S by recruiting an E3 ubiquitin ligase. This molecular tool facilitates the modulation of estrogen signaling pathways, providing a research application in the study of hormone-driven cancers. By utilizing a combination of a linker and a protein-binding domain, it enhances the degradation efficiency of the mutant receptor, enabling insights into the role of ERα Y537S in tumor biology and potential therapeutic strategies.
  14. PROTACs

    PROTAC BRD9 Degrader-2 is a bifunctional degrader that targets the BRD9 protein utilizing the PROTAC mechanism. This compound facilitates the targeted ubiquitination and subsequent degradation of BRD9, thus significantly influencing cancer-related pathways. It is instrumental in cancer research, particularly in studies aimed at understanding the role of BRD9 in tumorigenesis and developing potential therapeutic strategies.
  15. SMARCA2 PROTAC degrader

    PROTAC SMARCA2 degrader-17 (compound I-290) is a potent PROTAC degrader designed to selectively target and degrade the SMARCA2 protein. It demonstrates effective degradation in A549 cells with a DC50 value of less than 100 nM and achieves a maximum degradation rate exceeding 90% after 24 hours of treatment. This reagent is valuable for research in cancer biology and the investigation of SMARCA2-related pathways.
  16. SMARCA2 PROTAC degrader

    PROTAC SMARCA2 degrader-16 (compound I-278) is a PROTAC designed to selectively degrade the SMARCA2 protein. It demonstrates significant biological activity by efficiently reducing SMARCA2 levels in A549 cells, achieving a DC50 value of less than 100 nM and a maximum degradation rate exceeding 90% after 24 hours of treatment. This compound is invaluable for research applications involving the modulation of SMARCA2 in cancer biology and therapeutic development.
  17. SMARCA2 Degrader

    PROTAC SMARCA2 degrader-25 is a potent heterobifunctional molecule that targets SMARCA2 for degradation via the proteasome pathway. With a DC50 value of less than 0.01 μM, this compound efficiently engages the target protein using a specific ligand, a link to facilitate the interaction, and an E3 ligase ligand to promote ubiquitination. Its high efficiency makes it a valuable tool in investigating the role of SMARCA2 in various biological processes and diseases.
  18. SMARCA2/4 PROTAC degrader

    PROTAC SMARCA2/4-degrader-32 is a PROTAC degrader that targets SMARCA2 and SMARCA4 proteins. It demonstrates effective degradation of these proteins in A549 cells, achieving DC50 values below 100 nM and a maximum degradation rate exceeding 90% after 24 hours of treatment. This compound is suitable for research applications focusing on the regulation of chromatin remodeling and its implications in various cancers.
  19. SMARCA2/4 PROTAC degrader

    PROTAC SMARCA2/4-degrader-16 (compound I-337) is a potent PROTAC degrader designed to selectively target and degrade SMARCA2 and SMARCA4 proteins. It demonstrates significant biological activity in A549 cells, achieving DC50 values of less than 100 nM and over 90% maximum degradation rate (Dmax%) after 24 hours of treatment. This compound is valuable for research applications focused on understanding the role of SMARCA2 and SMARCA4 in tumor biology and for exploring targeted protein degradation strategies.
  20. ERα Degrader

    PROTAC ERα Degrader-8 is a highly potent degrader of estrogen receptor alpha (ERα), demonstrating a DC50 value of 6 nM in MCF7 breast cancer cells. This compound harnesses the proteolysis-targeting chimera (PROTAC) technology to selectively induce the degradation of ERα, facilitating studies on estrogen signaling pathways and potential therapeutic interventions in hormone-driven cancers. Its application in research provides insight into targeting ERα-related pathways for cancer treatment strategies.
  21. Ribonuclease-Targeting Chimeras

    F1-RIBOTAC is a ribonuclease-targeting chimera (RIBOTAC) that functions by enhancing the activity of RNase L to selectively degrade QSOX1-a mRNA. This targeted approach results in a significant reduction in QSOX1-a expression, making F1-RIBOTAC a valuable tool for cancer research. Its design integrates RNA ligands and RNase L ligands, providing a novel modality for studying RNA degradation pathways in malignant cells.
  22. SMARCA2 PROTAC degrader

    PROTAC SMARCA2 degrader-12 is a molecule specifically designed to induce degradation of the SMARCA2 protein. This PROTAC exhibits potent biological activity, effectively degrading SMARCA2 proteins in A549 cells with a DC50 value of less than 100 nM and achieving over 90% maximum degradation after 24 hours of treatment. This reagent is suitable for research applications focusing on targeted protein degradation and the functional analysis of SMARCA2 in cancer biology.
  23. ERα Degrader

    PROTAC ERα Degrader-10 (Compound 160a) is a potent degrader targeting estrogen receptor alpha (ERα) with a DC50 of 0.37-1.1 nM in cell lines such as MCF7, T47D, and CAMA-1. This compound effectively induces degradation of ERα, demonstrating significant antitumor activity in mouse models. It is a valuable tool for investigating ERα-related signaling pathways and exploring therapeutic strategies for ERα-positive breast cancers.
  24. Molecular Glue Degrader

    (S)-dHTC1 is a molecular glue degrader that targets the transcriptional co-activator ENL. This compound exhibits high-affinity binding to the E3 ligase upon forming the ENL:dHTC1 complex, with an IC50 value of 93 nM. In MV4;11 cells, (S)-dHTC1 effectively degrades ENL, demonstrating a DC50 value of 26 nM. This reagent is valuable for studying mechanisms in acute myeloid leukemia.
  25. AR PROTAC Degrader

    TD-802 is an androgen receptor (AR) PROTAC degrader that demonstrates substantial microsomal stability. It exhibits notable antitumor efficacy in vivo, making it a valuable tool for investigating metastatic castration-resistant prostate cancer. This compound is essential for research aimed at understanding AR modulation and its impacts on cancer progression.
  26. SMARCA2/4 Degrader

    PROTAC SMARCA2/4-degrader-35 is an efficient degrader targeting the SMARCA2 and SMARCA4 proteins, demonstrating a DC50 of less than 2.5 nM. This compound promotes the ubiquitination and subsequent degradation of the target proteins via the recruitment of E3 ligases. Its potent biological activity makes it valuable for research applications focused on epigenetics and cancer biology, particularly in studies targeting the modulation of chromatin remodeling complexes.
  27. SMARCA2 PROTAC degrader

    PROTAC SMARCA2 degrader-14 is a targeted protein degradation compound designed to selectively degrade the SMARCA2 protein. Demonstrating a DC50 value of less than 100 nM, it achieves maximum degradation rates exceeding 90% in A549 cells following a 24-hour treatment. This reagent serves as a valuable tool for research applications focused on elucidating the role of SMARCA2 in various biological processes and therapeutic contexts.
  28. HaloTag PROTAC Degrader

    Chlorohexane-PEG-clozapine is a HaloTag PROTAC degrader that employs clozapine to selectively target and promote the degradation of HaloTag fusion proteins. It effectively reduces luminescence intensity and decreases the protein levels of Halo-Eluc, facilitating the study of target protein dynamics and function. This reagent is valuable for research applications focusing on targeted protein degradation and modulation of protein levels in cellular systems.
  29. MAGE-A3 PROTAC Degrader

    KL-465 is a PROTAC degrader designed to target and degrade MAGE-A3, exhibiting a DC50 of 2 μM in HeLa cells. This compound effectively inhibits the viability of MAGE-A3 positive cancer cell lines, including HCT116, A375, and HeLa, making it a valuable tool for cancer research. Its unique mechanism facilitates targeted protein degradation, offering potential insights into therapeutic interventions for tumors expressing MAGE-A3.
  30. SMARCA2/4 PROTAC Degrader

    PROTAC SMARCA2/4 degrader-41 is a potent degrader targeting the SMARCA2 and SMARCA4 proteins, exhibiting DC50 and IC50 values both below 0.1 μM. This compound facilitates the selective degradation of these ATP-dependent chromatin remodelers, making it a valuable tool for studying SMARCA2/4-related or SMARCA2/4-deficient cancers. Its application in cancer research can aid in elucidating the role of these proteins in tumorigenesis and therapeutic resistance.
  31. DYRK2 PROTAC Degrader

    PROTAC DYRK2 degrader 1 is a selective degrader targeting DYRK2, functioning through the ubiquitin-proteasome system. It exhibits DC50 values of 1.607 μM in MDA-MB-231 cells and 3.265 μM in HeLa cells, effectively inducing DYRK2 degradation. This compound is valuable for research focused on triple-negative breast cancer and cervical cancer, facilitating the exploration of targeted protein degradation mechanisms in these malignancies.
  32. PROTAC ERα Degrader

    PROTAC ERα Degrader-7 is a highly effective degradative compound specifically targeting estrogen receptor alpha (ERα). It operates through a PROTAC mechanism and exhibits a DC50 value of 0.000006 µM, demonstrating its potent biological activity. This compound features a cereblon-binding moiety and an ERα-binding ligand, characterized by a benzofused partially saturated six-membered carbocyclic or heterocyclic ring structure. PROTAC ERα Degrader-7 is valuable for research applications focused on hormone signaling and therapeutic strategies in hormone-responsive cancers.
  33. MEKs Degrade PROTAC

    Folate-MS432 selectively targets MEKs through a PROTAC mechanism, facilitating their degradation in a folate receptor-dependent manner. This compound demonstrates significant efficacy in cancer cells, providing a powerful tool for investigating the role of MEK degradation in tumor biology. Folate-MS432 is valuable for research applications focusing on therapeutic strategies that manipulate signaling pathways in cancer treatment.
  34. PROTAC ERα Degrader

    NEP168 is a potent ERα PROTAC degrader that utilizes the GID4 E3 ligase for targeted protein degradation. This compound effectively reduces ERα levels, offering valuable insights into estrogen receptor-related signaling pathways. NEP168 serves as a crucial tool for investigating breast cancer biology and may aid in the development of novel therapeutic strategies.
  35. SMARCA2/4 PROTAC degrader

    PROTAC SMARCA2/4-degrader-7 is a selective protein degrader that targets SMARCA2 and SMARCA4 proteins. Demonstrating effective degradation in A549 cells, it achieves DC50 values of less than 100 nM and results in more than 90% degradation after 24 hours of treatment. This compound serves as a valuable tool for investigating the roles of SMARCA2 and SMARCA4 in cancer biology and other research applications involving epigenetic regulation.
  36. SMARCA2/4 PROTAC degrader

    PROTAC SMARCA2/4-degrader-22 is a targeted protein degradation reagent designed to selectively degrade SMARCA2 and SMARCA4 proteins. This compound effectively reduces SMARCA2 and SMARCA4 levels in A549 cells, achieving DC50 values of less than 100 nM and exceeding 90% maximum degradation rate after 24 hours of treatment. It is a valuable tool for research into the role of these proteins in various biological processes and disease states.
  37. mini-PROTAC ERRα Degrader

    Arg-TERRα is a mini-PROTAC designed to target estrogen-related receptor alpha (ERRα). This compound facilitates the degradation of ERRα via the N-end rule pathway, effectively suppressing the proliferation and migration of MCF7 breast cancer cells. Arg-TERRα serves as a valuable tool for investigating the role of ERRα in breast cancer research and therapeutic development.
  38. PROTACs

    PROTAC BRD9 Degrader-3 is a bifunctional degrader targeting BRD9 through the PROTAC mechanism, facilitating targeted protein degradation. This compound exhibits potent biological activity by selectively degrading BRD9, which plays a critical role in various cancer pathways. It is intended for use in cancer research to elucidate the functional significance of BRD9 and to explore novel therapeutic strategies in oncology.
  39. ITK Degrader

    ITK Degrader 2 is a PROTAC-based compound that specifically targets and degrades the interleukin-2-inducible T-cell kinase (ITK) with a DC50 value of less than 10 nM. In pharmacokinetic studies in mice, this orally active degrader demonstrates a maximum concentration (Cmax) of 0.87 μM and achieves peak plasma levels (Tmax) at 2 hours post-administration. At a dosage of 90 mg/kg, ITK Degrader 2 effectively reduces ITK levels by 20% within 6 hours, making it a valuable tool for exploring ITK-related signaling pathways and their implications in immune responses.
  40. BRD9 PROTAC Degrader

    PROTAC BRD9 Degrader-8 is a selective BRD9 PROTAC degrader that operates through targeted protein degradation, exhibiting a DC50 of 16 pM. This compound effectively induces cell cycle arrest in the G1 phase and promotes apoptosis, making it a valuable tool for studies focused on acute myeloid leukemia and diffuse large B-cell lymphoma. Its mechanism provides a unique approach to modulating BRD9 levels in therapeutic research.
  41. PROTAC degrader

    PROTAC SMARCA2/4-degrader-11 is a targeted protein degradation tool that specifically promotes the degradation of the SMARCA family of proteins. With a DC50 value of less than 100 nM, this compound effectively induces the destruction of SMARCA2 and SMARCA4. Its unique design features an inhibitor component, a linker, and an E3 ligase ligand, facilitating the targeted removal of these proteins, making it a valuable reagent for research into cancer biology and epigenetic regulation.
  42. SMARCA2 PROTAC degrader

    PROTAC SMARCA2 degrader-15 is a targeted PROTAC that selectively degrades the SMARCA2 protein. Demonstrating a DC50 value of less than 100 nM, this compound achieves over 90% maximum degradation (Dmax%) within 24 hours in A549 cells. Its ability to modulate SMARCA2 levels makes it a valuable tool for research exploring the role of this protein in cancer biology and epigenetic regulation.
  43. Proteolysis Targeting Chimera

    BT-PROTAC is a proteolysis targeting chimera (PROTAC) that enables the targeted degradation of specific proteins through a bioorthogonal activation mechanism. By accurately controlling PROTAC activity, it facilitates the selective modulation of protein levels within cells. This compound is valuable for research applications focused on the study of protein function, cellular signaling pathways, and the development of targeted therapeutic strategies.
  44. AR PROTAC Degrader

    A031 is a potent PROTAC degrader targeting the androgen receptor (AR), demonstrating an IC50 value of less than 0.25 μM for effective AR protein degradation. This compound has shown a significant inhibitory effect on tumor growth in zebrafish models of human prostate cancer (VCaP). A031 is a valuable tool for investigating AR-mediated signaling pathways and potential therapeutic strategies in prostate cancer research.
  45. PROTAC HMGCR Degrader

    PROTAC HMGCR Degrader-2 selectively targets HMG-CoA reductase (HMGCR) for degradation through the VHL-dependent ubiquitin-proteasome system, exhibiting an IC50 value of 0.25 μM and a DC50 of 0.12 μM in Insig-silenced HepG2 cells. This compound effectively reduces cellular cholesterol levels, making it valuable for research related to hyperlipidemia. Its mechanism of action enables precise modulation of cholesterol biosynthesis pathways, providing insights into lipid metabolism and potential therapeutic interventions.
  46. SMARCA2/4 PROTAC degrader

    PROTAC SMARCA2/4-degrader-23 is a targeted proteolysis-targeting chimera (PROTAC) designed to degrade SMARCA2 and SMARCA4 proteins. This compound effectively induces degradation of both targets in A549 cells, exhibiting a DC50 of less than 100 nM and achieving a maximum degradation rate exceeding 90% after 24 hours of treatment. It is suitable for use in studies aimed at understanding the functional roles of SWI/SNF chromatin remodeling complexes in cancer and other disease models.
  47. SMARCA2 PROTAC degrader

    PROTAC SMARCA2 degrader-10 is a targeted protein degrader that specifically engages and promotes the degradation of SMARCA2. This compound demonstrates effective degradation of SMARCA2 proteins in A549 cells, achieving a DC50 value of less than 100 nM and a maximum degradation rate exceeding 90% after 24 hours of treatment. It serves as a valuable tool for research applications focused on elucidating the biological roles of SMARCA2 and its implications in cancer biology and therapeutics.
  48. SMARCA2 PROTAC degrader

    PROTAC SMARCA2 degrader-6 (compound I-427) is a PROTAC agent specifically designed to target and induce the degradation of SMARCA2 proteins. This compound effectively degrades SMARCA2 in A549 cells, achieving a DC50 value of less than 100 nM and demonstrating a maximum degradation rate exceeding 90% within 24 hours of treatment. It serves as a powerful tool for investigating the role of SMARCA2 in various biological processes and potential therapeutic applications in cancer research.
  49. CRBN Degrader PROTAC

    ZXH-4-137 is a potent and selective CRBN degrader that utilizes the PROTAC mechanism to promote targeted protein degradation. This compound effectively recruits the E3 ubiquitin ligase CRBN to facilitate the degradation of specific proteins, making it a valuable tool for studying protein function and regulation. It has applications in cellular assays and therapeutic research aimed at diseases associated with protein homeostasis.
  50. Cbl-b PROTAC Degrader

    PROTAC Cbl-b-IN-1 is a potent Cbl-b PROTAC degrader, exhibiting a DC50 of less than 30 nM. This compound effectively induces the targeted degradation of the Cbl-b protein, making it a valuable tool for cancer research. Its ability to modulate protein levels through degradation pathways allows for in-depth studies of Cbl-b's role in tumor biology and therapeutic interventions.

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