PROTAC

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  1. ADC/PROTAC Linker

    Propargyl-PEG8-NHS ester is a PEG-based linker specifically designed for antibody-drug conjugates (ADCs) and PROTACs. Its primary mechanism involves enabling the synthesis of these bioconjugates through a cleavable linker. This compound features an alkyne group that facilitates click chemistry, specifically the copper-catalyzed azide-alkyne cycloaddition (CuAAc), allowing for efficient conjugation with azide-containing molecules. It is a valuable tool for researchers in drug development and bioconjugation studies.
  2. ADC/PROTAC Linker

    Propargyl-PEG6-acid is a PEG-based linker primarily utilized in the synthesis of proteolysis-targeting chimeras (PROTACs) and antibody-drug conjugates (ADCs). This cleavable linker facilitates the formation of ADCs and enables targeted protein degradation via a click chemistry reaction, leveraging its alkyne group for copper-catalyzed azide-alkyne cycloaddition (CuAAc). Its versatile applications in chemical biology make it a valuable tool for research in targeted therapeutics and bioconjugation strategies.
  3. PROTAC Linker

    Fmoc-NH-PEG9-CH2CH2COOH is a cleavable linker designed for use in the synthesis of antibody-drug conjugates (ADCs) and PROTACs. This PEG-based compound facilitates the conjugation of therapeutic agents to targeted antibodies, enhancing efficacy and selectivity in drug delivery. Its unique structure allows for the effective modulation of protein degradation pathways, making it valuable for research applications in targeted protein degradation and drug development.
  4. ADC/PROTAC Linker

    Propargyl-PEG8-NH2 is a PEG-based linker primarily used in antibody-drug conjugates (ADCs) and PROTAC synthesis. This non-cleavable linker enhances the stability of ADCs while facilitating the targeted delivery of therapeutic agents. Additionally, its alkyne functional group allows for copper-catalyzed azide-alkyne cycloaddition (CuAAc), making it a valuable tool in click chemistry applications for bioconjugation and drug development.
  5. PROTAC Linker

    Bis-PEG9-acid is a PEG-based linker designed for use in the synthesis of PROTACs (Proteolysis Targeting Chimeras). This compound features a cleavable structure, making it suitable for the development of antibody-drug conjugates (ADCs). Its unique properties facilitate targeted degradation of proteins, enabling efficient research in drug discovery and therapeutic development.
  6. PROTAC Linkers

    Azido-PEG4-CH2-Boc functions as a cleavable linker primarily utilized in the synthesis of antibody-drug conjugates (ADCs) and PROTACs. This versatile reagent incorporates a PEG spacer and an azide group, allowing it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc) as well as strain-promoted alkyne-azide cycloaddition (SPAAC) reactions. Its effective application in the development of novel bioconjugates and protein degradation-based therapeutic strategies makes it a valuable tool in chemical biology and drug development research.
  7. PROTAC/ADC Linker

    NH2-PEG5-OH is a PEG-based linker designed for use in the synthesis of proteolysis-targeting chimeras (PROTACs) and antibody-drug conjugates (ADCs). This non-cleavable linker, incorporating a five-unit polyethylene glycol (PEG) structure, enhances the stability and solubility of biologically active compounds. Researchers utilize NH2-PEG5-OH to facilitate targeted degradation of proteins or deliver cytotoxic agents via ADCs, improving therapeutic efficacy in various applications.
  8. PROTAC Linkers

    N3-PEG3-CH2CH2-Boc is a cleavable linker designed for use in PROTAC synthesis, specifically serving as a 3-unit polyethylene glycol (PEG) intermediary. This compound facilitates the formation of antibody-drug conjugates (ADCs) and supports click chemistry applications through its azide group. It readily participates in copper-catalyzed azide-alkyne cycloaddition (CuAAc) with alkyne-functionalized molecules and can also engage in strain-promoted alkyne-azide cycloaddition (SPAAC) with DBCO or BCN groups, proving valuable in diverse chemical research applications.
  9. ADC/PROTAC Linker

    Propargyl-PEG6-NHS ester is a cleavable linker designed for the synthesis of antibody-drug conjugates (ADCs) and PROTACs. This PEG-based reagent features an alkyne group that enables copper-catalyzed azide-alkyne cycloaddition (CuAAc), facilitating the conjugation of biomolecules. Its versatility as a click chemistry reagent enhances the development of targeted therapies in chemical biology and drug discovery applications.
  10. ADC/PROTAC Linker

    Amino-PEG5-C2-acid is a PEG-based linker designed for use in the synthesis of PROTACs and non-cleavable antibody-drug conjugates (ADCs). This compound facilitates the conjugation of active pharmaceutical ingredients to antibodies, thereby enhancing target specificity and therapeutic efficacy. Its unique structure allows for optimal stability and performance in bioconjugation applications, making it a valuable tool for researchers in drug development and targeted therapy.
  11. PROTAC/ADC Linker

    Amino-PEG4-CH2COOH is a PEG-based linker designed for use in the synthesis of proteolysis-targeting chimeras (PROTACs) and serves as a non-cleavable four-unit PEG linker for antibody-drug conjugates (ADCs). This compound facilitates the formation of stable conjugates, thereby enhancing the delivery of therapeutic agents to targeted cells. Its unique properties support research applications in targeted protein degradation and ADC development, contributing to advancements in cancer therapy and drug efficacy.
  12. PROTAC Linkers

    NH-bis-PEG2 is a non-cleavable linker featuring a two-unit polyethylene glycol (PEG) structure, primarily utilized in the development of antibody-drug conjugates (ADCs). This PEG-based linker is also applicable in the synthesis of PROTACs, facilitating targeted protein degradation. Its chemical properties allow for improved solubility and stability, making it a valuable tool in drug development and biochemical research.
  13. ADC/PROTAC Linker

    N-Boc-PEG7-alcohol is a PEG-based linker primarily utilized in the synthesis of PROTACs and antibody-drug conjugates (ADCs). This cleavable linker facilitates targeted drug delivery by enhancing the solubility and stability of therapeutic compounds. Its versatile applications in chemical biology make it a valuable tool for researchers aiming to develop novel targeted therapies.
  14. ADC/PROTAC Linker

    m-PEG10-amine is a non-cleavable 10 unit polyethylene glycol (PEG) linker designed for use in the synthesis of antibody-drug conjugates (ADCs) and PROTACs (Proteolysis Targeting Chimeras). This linker enhances the solubility and stability of conjugated biomolecules, facilitating targeted delivery and improved therapeutic efficacy. It is particularly valuable in research applications focusing on ADC development and targeted protein degradation strategies.
  15. PROTAC Linkers

    Propargyl-PEG4-Tos is a PEG-based linker specifically designed for the synthesis of PROTACs (proteolysis-targeting chimeras). It serves as a cleavable linker in antibody-drug conjugates (ADCs), facilitating targeted delivery of therapeutic agents. This compound features an alkyne group that enables copper-catalyzed azide-alkyne cycloaddition (CuAAc), allowing for efficient conjugation with azide-containing molecules. Its versatile applications make it a valuable tool in chemical biology and drug development research.
  16. ADC/PROTAC Linker

    N-Boc-PEG6-alcohol is a PEG-based linker designed for antibody-drug conjugate (ADC) and PROTAC applications. This cleavable linker facilitates the synthesis of PROTACs, allowing for targeted degradation of specific proteins. Its unique structure provides enhanced solubility and stability, making it suitable for various biochemical studies focused on targeted therapies and protein regulation.
  17. SMARCA2 PROTAC Degrader

    PROTAC SMARCA2 degrader-35 is a selective degrader targeting SMARCA2 with a DC50 potency of less than 0.1 μM. This compound exhibits significant anticancer activity by regulating cell proliferation and growth, primarily through mechanisms of cell cycle arrest and inhibition of DNA replication in SMARCA4-deleted cancer cells. It is a valuable tool for research focused on targeted protein degradation and its implications in cancer therapy.
  18. PROTAC Linker

    N-(Azido-PEG3)-N-Fluorescein-PEG3-acid is a PEG-based linker utilized in PROTAC technology, featuring azide, fluorescein, and carboxylic acid functionalities. This compound serves as a versatile click chemistry reagent capable of participating in copper-catalyzed azide-alkyne cycloaddition (CuAAc) with alkyne-containing partners, as well as strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with DBCO or BCN groups. Its unique properties make it suitable for applications in tandem with targeted protein degradation and fluorescent labeling studies in chemical biology.
  19. PROTAC Linker

    Biotin-PEG-azide (MW 1000) is a PEG-based linker designed for PROTAC synthesis, featuring an azide functional group. This versatile compound can participate in copper-catalyzed azide-alkyne cycloaddition (CuAAC) reactions with alkyne-containing molecules, as well as in strain-promoted alkyne-azide cycloaddition (SPAAC) with DBCO or BCN functionalized compounds. Its unique properties make it suitable for applications in targeted protein degradation research and other areas of chemical biology.
  20. ADC/PROTAC Linkers

    Glucocorticoid receptor agonist-1 phosphate(2,6-difluoro) Ala-Ala-Br serves as a versatile drug-linker conjugate for antibody-drug conjugate (ADC) applications. This reagent enables the synthesis of conjugates targeting the CD40 antigen, facilitating the development of targeted therapies. Its unique structure supports the design of PROTACs and other innovative bio-conjugates, contributing to advances in cancer research and immunotherapy.
  21. Chk1 PROTAC Degrader

    PROTAC Chk1 degrader-1 is a selective Chk1-targeting PROTAC that facilitates the recruitment of the Cereblon E3 ligase to promote ubiquitination and subsequent proteasomal degradation of Chk1. This compound effectively induces Chk1 degradation in malignant melanoma cells, demonstrating a robust biological activity without exhibiting a hook effect. PROTAC Chk1 degrader-1 is suitable for research applications focused on understanding the role of Chk1 in malignant melanoma and exploring targeted degradation strategies in cancer therapy.
  22. Molecular Glue BRD4 Degrader

    BRD4 degrader-1 is a monovalent, covalent molecular glue that specifically targets BRD4, a key regulator in various cellular processes. By engaging DCAF16, an E3 ubiquitin ligase, this compound facilitates the degradation of both long and short isoforms of BRD4 within the cellular context. Its mechanism of action makes BRD4 degrader-1 a valuable tool for research applications aimed at understanding and manipulating BRD4-related pathways in cancer and other diseases.
  23. BRD4 Degrader

    MMH1 is a novel BRD4 molecular glue degrader that effectively recruits the CUL4 and DCAF16 ligases to the second bromodomain of BRD4 (BRD4BD2). This targeted degradation mechanism allows for the selective reduction of BRD4 levels, which is crucial for studying its role in various biological processes. MMH1 is particularly useful in research applications focusing on cancer biology and epigenetic regulation, enabling the exploration of therapeutic strategies targeting BRD4-associated pathways.
  24. BRD4 Degrader

    BRD4 degrader-3 is a selective bromodomain-containing protein 4 (BRD4) degrader, showcasing potent activity with IC50 values of 15.5 nM and 12.3 nM for BRD4-BD1 and BRD4-BD2, respectively. This compound employs the PROTAC technology to facilitate targeted degradation of BRD4. Additionally, it features an alkyne functional group that enables copper-catalyzed azide-alkyne cycloaddition (CuAAc), making it a valuable tool for chemical biology applications in studying BRD4-related pathways and functions.
  25. BRD9 PROTAC Degrader

    dBRD 9-A is a selective BRD9 PROTAC degrader that targets the E3 ubiquitin ligase CRBN for the near-complete degradation of BRD9. This compound disrupts BRD9 chromatin binding on a genome-wide scale, leading to downregulation of oncogenic transcriptional programs driven by SS18-SSX and the depletion of GBAF complex members from SS18-SSX complexes. dBRD 9-A also induces cell cycle arrest and promotes apoptosis in synovial sarcoma cells, making it a valuable tool for research focused on synovial sarcoma.
  26. PROTAC BRD4 Degrader

    TD-428 is a potent PROTAC designed to target and degrade the BRD4 protein via its connection to Cereblon ligands. With a DC50 value of 0.32 nM, TD-428 exhibits high specificity for BRD4 degradation. This compound combines TD-106, a ligand for CRBN, with JQ1, a BET inhibitor, facilitating effective degradation of BET proteins. TD-428 is valuable for research applications involving cancer biology and epigenetic regulation.
  27. BRD4 PROTAC Degrader

    L1BC8 is a BRD4 PROTAC degrader that exhibits significant anticancer activity through targeted degradation of the BRD4 protein. This compound functions as a drug-linker conjugate for antibody-drug conjugates (ADCs), enabling the synthesis of BRD4-degrader antibody conjugates. The resulting conjugates demonstrate potent, antigen-dependent BRD4 degradation and antiproliferative effects in cellular assays, making L1BC8 a valuable tool for cancer research and therapeutic development.
  28. Molecular Glue

    AMPTX-1 is a molecular glue that functions as a selective, reversibly covalent degrader of BRD9, promoting its recruitment to the E3 ubiquitin ligase DCAF16. This compound exhibits significant activity in inducing proteasomal degradation of BRD9, making it a valuable tool for research involving chromatin regulation and cellular signaling pathways. AMPTX-1 can be utilized in studies focused on targeted protein degradation and the modulation of BRD9-related biological processes.
  29. BRD9 Degrader

    PROTAC BRD9 Degrader-7 is a selective BRD9-targeting PROTAC that induces BRD9 degradation through the ubiquitin-proteasome pathway, demonstrating a DC50 of 1.02 nM. This compound effectively inhibits cell proliferation in MV4-11 acute myeloid leukemia cells, making it a valuable tool for research in hematologic malignancies and related disorders. Its capacity to modulate BRD9 levels positions it as a promising candidate for studies aimed at understanding the role of this protein in cancer biology.
  30. SMARCA2/SMARCA4 Degrader

    G-6599 is a monovalent degrader targeting SMARCA2 and SMARCA4, known for its role in regulating chromatin remodeling. This compound covalently binds to a specific cysteine residue in the E3 ligase FBXO22, facilitating the formation of a ternary complex with SMARCA2 and SMARCA4, leading to their efficient degradation through the ubiquitin-proteasome pathway. G-6599 is relevant for research in androgen-dependent prostate cancer and mutant non-small cell lung cancer, providing valuable insights into therapeutic interventions.
  31. SMARCA2 Degrader

    YDR1 is a potent SMARCA2 degrader that functions as a PROTAC, exhibiting a DC50 of 7.7 nM. This compound is particularly relevant for research into SMARCA4 mutant cancers, facilitating targeted degradation of SMARCA2. It offers valuable insights into the molecular mechanisms underlying these cancers and aids in the development of novel therapeutic strategies.
  32. PROTAC BRD4 Degrader

    CCW 28-3 is a PROTAC that specifically targets BRD4 for degradation through a proteasome- and RNF4-dependent mechanism. This compound facilitates the targeted removal of BRD4, a critical regulator of gene expression linked to various cancers. Its application in research includes studying the role of BRD4 in transcriptional regulation and therapeutic interventions aimed at modulating oncogenic pathways.
  33. PROTAC BRD4 Degrader

    PROTAC BRD4 Degrader-9 is a bifunctional degrader targeting the BRD4 protein through a ligase-dependent mechanism using von Hippel-Lindau. It exhibits potent biological activity, effectively degrading BRD4 in PC3 prostate cancer cells with a DC50 of 0.86 nM when conjugated with STEAP1 antibodies and 7.6 nM with CLL1 antibodies. This compound is valuable for research into targeted protein degradation and therapeutic strategies against BRD4-mediated oncogenic processes.
  34. CBP/p300 PROTAC Degrader

    Thalidomide-NH-CBP/p300 ligand 2 is a PROTAC-based degrader that targets the CBP and p300 proteins. This compound facilitates the selective degradation of these transcriptional coactivators, which are implicated in various cancers and other diseases. Its application in research includes the elucidation of the roles of CBP and p300 in transcriptional regulation and therapeutic development for conditions influenced by these proteins.
  35. PROTAC ERRα Degrader

    PROTAC_ERRα is a targeted degrader of the estrogen-related receptor alpha (ERRα), employing a proteolysis-targeting chimera (PROTAC) mechanism for enhanced specificity. This compound induces over 80% proteasomal degradation of ERRα in MCF-7 cells, with a DC50 value of 100 nM. PROTAC_ERRα serves as a valuable tool for investigating the biological functions of ERRα in cancer research and for therapeutic development aimed at ERRα-related pathways.
  36. PROTAC BRD4 Degrader

    PROTAC BRD4 Degrader-2 is a proteolysis-targeting chimera (PROTAC) that selectively targets BRD4 and Cereblon. With an IC50 of 14.2 nM against the BRD4 BD1 domain, this compound effectively induces proteasomal degradation of BRD4. It is valuable for research applications investigating the role of BRD4 in transcription regulation, cancer biology, and other diseases associated with aberrant gene expression.
  37. PROTAC BRD4BD1L94V Degrader

    XY-06-007 is a selective and potent bump-and-hole (B&H) PROTAC that degrades BRD4BD1L94V. It exhibits a degradation concentration (DC50) of 10 nM at 6 hours, effectively targeting BRD4BD1L94V without degrading off-target proteins. With favorable pharmacokinetic properties, XY-06-007 is suitable for in vivo studies and serves as a valuable tool for research into BRD4-related pathways and therapeutic applications.
  38. SMARCA2 PROTAC Degrader

    SMD-3236 is a SMARCA2 PROTAC degrader that effectively induces the degradation of the SMARCA2 protein through proteasome- and ubiquitin-dependent mechanisms, achieving a DC50 of 0.5 nM and Dmax of 98%. It demonstrates an IC50 of 42.2 nM against human SMARCA2, providing significant growth inhibition in SMARCA4-deficient cancer cells. SMD-3236 has shown profound and sustained depletion of SMARCA2 in tumor tissues and suppresses tumor growth in relevant xenograft models. This reagent is valuable for research focusing on SMARCA4-deficient cancers, including melanoma, non-small cell lung cancer, and acute myeloid leukemia.
  39. PROTAC BRD4 Degrader

    PROTAC BRD4 Degrader-10 is a proteolysis-targeting chimera (PROTAC) designed to selectively degrade the BRD4 protein via recruitment of the von Hippel-Lindau (VHL) E3 ligase. This compound exhibits significant biological activity in degrading BRD4 in PC3 prostate cancer cells, demonstrating effective DC50 values of 1.3 nM when conjugated with STEAP1 antibodies and 18 nM with CLL1 antibodies. This reagent is valuable for studying the role of BRD4 in cancer biology and exploring targeted degradation strategies in therapeutic applications.
  40. BRD9 degrader

    PROTAC BRD9 Degrader-6 is a highly effective degrader targeting BRD9, exhibiting an IC50 of 0.13 nM. This compound selectively induces proteolysis of BRD9, facilitating the study of diseases associated with the BAF complex. It is a valuable tool for researchers investigating the role of BRD9 in various biological contexts and its potential therapeutic applications.
  41. SMARCA2/4 PROTAC Degrader

    PROTAC SMARCA2/4-degrader-18 is a dual-target PROTAC degrader that selectively degrades the catalytic subunits SMARCA2 and SMARCA4 of the SWI/SNF complex. It exhibits potent degradation activity with DC50 values of less than 100 nM in A549 cells for SMARCA2 and MV411 cells for SMARCA4. This reagent is useful for investigating the functional roles of SMARCA2 and SMARCA4 in cellular processes and may provide new insights into therapeutic strategies targeting chromatin remodeling in cancer research.
  42. BRD PROTAC Degrader

    PROTAC BRD4 Degrader-26 is a photo-regulated PROTAC designed to selectively degrade BRD4 through a photocleavable linker. This compound achieves an impressive 80% degradation of BRD4 at a concentration of 1 μM, demonstrating significant potency. The degradation process can be controlled by UV light, allowing for precise temporal regulation of BRD4 levels. It is an essential tool for researchers investigating the role of BRD4 in various biological pathways and its potential as a therapeutic target.
  43. SMARCA2 Degrader

    PROTAC SMARCA2/4-degrader-10 targets the selective degradation of SMARCA2, exhibiting a DC50 value of less than 100 nM. This compound serves as a valuable tool in cancer research, facilitating studies on tumor biology and the therapeutic potential of targeting the BRG1/BRM-associated factor complex. The design incorporates a ligand linked to a VHL ligand, enhancing the efficacy of the degrader in cellular environments.
  44. PROTAC BRD3 Degrader

    PROTAC BRD3 Degrader-1 is a potent and selective proteolysis-targeting chimera (PROTAC) designed to degrade BRD3. Its mechanism involves the targeted degradation of BRD3, leading to the downregulation of H3K18ac while sparing BRD2 and BRD4. This compound demonstrates significant efficacy in reducing intraocular inflammation in the experimental autoimmune uveitis mouse model and inhibits pro-inflammatory responses in microglial cells, making it a valuable tool for uveitis research.
  45. SMARCA2/4 Molecular Glue Degrader

    SMARCA2/4 degrader-1 is a molecular glue degrader specifically targeting SMARCA2 and SMARCA4, exhibiting a DC50 value of 2.2 nM for SMARCA4. This compound functions by covalently bridging CUL4DCAF16 and CRL1FBXO22, leading to the efficient degradation of SMARCA2 and SMARCA4 proteins. It is utilized in research to understand the roles of these proteins in various biological processes and disease states, particularly in cancer biology and epigenetic regulation.
  46. SMARCA2 PROTAC Degrader

    PROTAC SMARCA2 degrader-21 is a targeted protein degradation compound that selectively degrades the SMARCA2 protein through the ubiquitin-proteasome system. It demonstrates potent biological activity with a DC50 value of 10-50 nM in A549 cells and exhibits even greater efficacy in MV411 cells, achieving a DC50 of less than 1 nM for SMARCA2 while showing limited degradation of SMARCA4 (DC50 >100 nM). This compound is useful for investigating the functional roles of SMARCA2 in cancer biology and therapeutic development.
  47. SMARCA2/4 Inhibitor

    SMARCA2-IN-8 is a selective inhibitor of the SWI/SNF chromatin remodeling complexes SMARCA2 and SMARCA4, exhibiting potent activity with IC50 values of 5 nM and 6 nM, respectively. This compound effectively inhibits the proliferation of SMARCA2-mutated cancer cells, specifically SKMEL5, with an AAC50 of 5 nM and downregulates SMARCA2-dependent KRT80 gene expression at an AAC50 of 10 nM. SMARCA2-IN-8 demonstrates substantial antitumor efficacy and favorable pharmacokinetic properties in preclinical mouse models, making it a valuable tool for investigating chromatin remodeling in cancer research.
  48. BRD4 PROTAC Degrader

    BRD4 degrader-6 is a dimeric PROTAC degrader targeting the BRD4 protein, demonstrating a DC50 of less than 0.1 μM. This compound facilitates the ubiquitination and subsequent degradation of BRD4, contributing to its anticancer properties. It serves as a valuable tool for studying BRD4-related pathways and potential therapeutic strategies in cancer research.
  49. SMARCA2/4 Degrader

    PROTAC SMARCA2/4-degrader-6, a targeted degrader of SMARCA2 and SMARCA4, employs a proteolysis-targeting chimeric approach to facilitate the degradation of these proteins. This compound demonstrates significant potential in cancer research by selectively lowering SMARCA2/4 levels, thereby disrupting oncogenic signaling pathways. Its unique structure includes a ligand for SMARCA2/4 and a VHL ligand to promote ubiquitination and subsequent proteasomal degradation, making it a valuable tool for elucidating the role of these proteins in tumor biology.
  50. E3 ligase ligand

    (S,R,S)-AHPC-Me-amide-C9-acid is an E3 ligase ligand-linker conjugate designed for targeted protein degradation applications. This reagent facilitates the synthesis of PROTAC SMARCA2 degrader-31, enabling investigations into the modulation of protein levels via the ubiquitin-proteasome system. Its unique structure enhances selectivity and efficacy in the degradation of specific target proteins, making it a valuable tool in chemical biology and therapeutic research.

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