PROTAC

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  1. PROTAC Linker

    Tert-Butyl 3-(3-iodopropyl)azetidine-1-carboxylate is an effective PROTAC linker designed for synthesizing Proteolysis Targeting Chimeras (PROTACs). This compound facilitates the degradation of specific proteins by promoting the recruitment of E3 ligases, providing a powerful tool for targeted protein modulation in biological research. It is applicable in studies focused on targeted protein degradation and can aid in the exploration of therapeutic strategies in various disease contexts.
  2. PROTAC Linker

    Methyl 8-oxooctanoate is a versatile PROTAC linker designed to facilitate the synthesis of proteolysis-targeting chimeras (PROTACs). It plays a crucial role in the development of novel therapeutic agents by linking target proteins to E3 ligases, thus promoting ubiquitination and degradation. This compound is essential for researchers investigating targeted protein degradation and its implications in various diseases.
  3. PROTAC Linker

    5-Iodopentan-1-ol is a versatile PROTAC linker that facilitates the design and synthesis of proteolysis-targeting chimeras (PROTACs). This compound plays a crucial role in creating potent and selective modulators of protein function by enabling the targeted degradation of specific proteins. It is essential for researchers focused on developing innovative therapeutic strategies in the fields of drug discovery and protein engineering.
  4. PROTAC Linker

    4-Chlorobutyronitrile is a reactive PROTAC linker utilized in the synthesis of proteolysis-targeting chimera (PROTAC) molecules. It facilitates the assembly of bifunctional small molecules designed to selectively degrade target proteins through the ubiquitin-proteasome system. This compound is valuable in the development of targeted protein degradation strategies for various therapeutic applications, including cancer research and neurological disorders.
  5. PROTAC Linker

    Piperidin-4-amine-C5-O-C1 is a PROTAC linker that facilitates the synthesis of proteolysis-targeting chimeras (PROTACs). It serves as a critical component in the development of bifunctional molecules designed to selectively degrade target proteins via the ubiquitin-proteasome system. This compound enables researchers to explore innovative therapeutic strategies in targeted protein degradation, advancing the field of molecular biology and drug discovery.
  6. PROTAC Linker

    3-(Azetidin-3-yl)propan-1-ol serves as a critical PROTAC linker, facilitating the creation of proteolysis-targeting chimeras (PROTACs). This compound contributes to the selective degradation of target proteins via the ubiquitin-proteasome system. It is utilized in various research applications focused on targeted protein degradation, advancing the understanding of protein function and therapeutic intervention in diseases.
  7. PROTAC Linker

    H2N-PEG4-Hydrazide is a PEG-based linker designed for use in the synthesis of Proteolysis Targeting Chimeras (PROTACs). This compound facilitates the conjugation of target proteins to E3 ligases, enhancing target degradation through the ubiquitin-proteasome system. H2N-PEG4-Hydrazide is essential for researchers exploring targeted protein degradation approaches in drug discovery and development.
  8. PROTAC Linker

    3-(Methylamino)propanoic acid serves as a PROTAC linker, facilitating the development of proteolysis-targeting chimeras (PROTACs) for targeted protein degradation. Its structure is optimized for conjugation, enhancing the efficacy of bioconjugates in research applications focused on protein modulation and cellular control mechanisms. This compound is instrumental in advancing drug discovery efforts aimed at novel therapeutic strategies.
  9. PROTAC Linker

    (S,R,S)-AHPC-PEG4-NHS ester is a PROTAC linker featuring an E3 ligase ligand connected by a PEG4 spacer, enhancing PROTAC drug discovery and development. Its NHS ester functionality allows for efficient coupling with amine-containing molecules, facilitating the formation of targeted protein degradation complexes. The PEG4 spacer further improves the solubility of the conjugated compounds, making this linker a valuable tool in chemical biology research and therapeutic applications.
  10. PROTAC Linker

    14-((tert-Butoxycarbonyl)amino)tetradecanoic acid serves as a versatile PROTAC linker, facilitating the construction of targeted protein degraders. This compound enables the formation of bifunctional molecules that can selectively recruit E3 ligases to target proteins for ubiquitination and subsequent degradation. Its application is pivotal in the development of innovative therapeutics aimed at modulating protein levels and investigating cellular pathways.
  11. PROTAC Linker

    4,4'-(Hexane-1,6-diylbis(oxy))dibenzonitrile serves as a PROTAC linker in the assembly of proteolysis-targeting chimeras (PROTACs). This compound facilitates the conjugation of protein ligands, enhancing selective protein degradation in targeted therapeutic applications. Its structural properties make it suitable for the development of innovative treatments in cancer and other diseases.
  12. PROTAC Linker

    Bn-PEG8-OBn is a polyethylene glycol (PEG) linker designed for use in the synthesis of proteolysis-targeting chimeras (PROTACs). This versatile linker facilitates the conjugation of target proteins to E3 ligases, enabling selective degradation of proteins of interest. Its application is significant in small molecule drug discovery and biological research, particularly in the development of targeted therapies.
  13. PROTAC Linker

    tert-Butyl 2-(piperidin-4-yl)acetate hydrochloride is a versatile PROTAC linker designed for the synthesis of Proteolysis Targeting Chimeras (PROTACs). This compound facilitates the recruitment of E3 ligases to target proteins, enabling targeted degradation pathways. Its role in PROTAC development makes it essential for research applications in targeted protein modulation and therapeutic interventions.
  14. PROTAC Linker

    OH-PEG3-Cl is a bifunctional linker designed for use in the synthesis of PROTACs (Proteolysis Targeting Chimeras). This reagent facilitates the conjugation of target proteins to an E3 ligase, enabling the degradation of specific proteins through the ubiquitin-proteasome system. Its application is crucial in chemical biology for the development of targeted protein degradation strategies that can be used in therapeutic research and drug discovery.
  15. PROTAC Linker

    Ethyl 7-oxoheptanoate serves as a versatile PROTAC linker, facilitating the synthesis of proteolysis-targeting chimeras (PROTACs). This compound plays a crucial role in enhancing the degradation of specific target proteins through the recruitment of E3 ligases. Its application extends to research in targeted protein degradation, making it valuable for studies in cancer biology and other disease mechanisms.
  16. PROTAC Linker

    1-Bromo-4-(4-bromobutyl)benzene acts as an effective PROTAC linker, facilitating the design and synthesis of Proteolysis Targeting Chimeras (PROTACs). This compound enables the selective degradation of target proteins by bridging an E3 ligase and a protein of interest, thereby enhancing the efficiency of targeted protein degradation studies. Its utility in the development of novel therapeutic strategies makes it valuable for research in drug discovery and protein regulation.
  17. PROTAC Linker

    3-Cyanocyclobutane-1-carboxylic acid serves as a synthetic linker for PROTAC (proteolysis-targeting chimera) development. This compound facilitates the formation of stable PROTACs, enabling targeted protein degradation by linking a target protein ligand to an E3 ligase ligand. Its unique structural properties make it valuable for research applications in protein modulation and therapeutics.
  18. PROTAC Linker

    Ethyl hex-5-ynoate serves as a PROTAC linker, facilitating the development of proteolysis-targeting chimeras (PROTACs). This compound is crucial for researchers aiming to create novel protein degraders that target specific proteins for degradation in cellular systems. Its versatility and effectiveness make it a valuable tool in chemical biology and drug discovery applications.
  19. PROTAC Linker

    tert-Butyl 4-(4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzoyl)piperazine-1-carboxylate is a specialized linker designed for the synthesis of PROTACs (proteolysis-targeting chimeras). This compound facilitates the targeted degradation of specific proteins by bridging E3 ubiquitin ligases with the target protein, enhancing the recruitment and subsequent ubiquitination. It is valuable in research applications focused on protein regulation and therapeutic discovery, particularly in cancer and neurodegenerative diseases.
  20. PROTAC Linkers

    HO-PEG8-CH2COOH is a polyethylene glycol (PEG)-based linker designed for use in the synthesis of Proteolysis Targeting Chimeras (PROTACs). This compound facilitates the conjugation of ligand molecules, enhancing the stability and solubility of PROTACs. HO-PEG8-CH2COOH is essential in chemical biology studies aimed at targeted protein degradation and provides a versatile tool for researchers developing novel therapeutic agents.
  21. PROTAC Linker

    2-Propargyl-(trans)-4-cyclohexanediamine functions as a versatile PROTAC linker, enabling the development of proteolysis-targeting chimeras (PROTACs). This compound facilitates the selective degradation of target proteins through the recruitment of E3 ubiquitin ligases, thereby enhancing the modulation of biological pathways. It is an essential tool in drug discovery and protein regulation research applications.
  22. PROTAC Linker

    3-Hydroxy-2,2,4,4-tetramethylcyclobutan-1-one oxime serves as a versatile PROTAC linker, facilitating the development of targeted protein degradation strategies. It enables the efficient combination of target proteins with E3 ligases, enhancing the design of PROTAC molecules. This compound is pivotal in biochemical research focused on modulating protein levels and exploring therapeutic potentials in various diseases.
  23. NR4A1 PROTAC Degrader

    NR-V04 is a selective degrader targeting NR4A1 via a PROTAC mechanism. It facilitates the formation of a ternary complex with NR4A1 and the VHL E3 ligase, promoting proteasome-dependent degradation of NR4A1. Through its action, NR-V04 has been shown to enhance the infiltration of tumor-associated B cells and effector memory CD8+ T cells while decreasing monocytic myeloid-derived suppressor cells within tumor microenvironments. This compound is valuable for research related to melanoma and colon cancer.
  24. CRBN Degrader

    ZXH-4-130 TFA is a potent and selective degrader of Cereblon (CRBN), functioning as a CRBN-VHL heterobifunctional protein degrader (PROTAC). This compound exhibits significant biological activity, inducing approximately 80% CRBN degradation at a concentration of 10 nM in MM1.S cells. ZXH-4-130 TFA is a valuable tool for investigating CRBN-mediated pathways and protein degradation mechanisms in various research applications.
  25. LDH-targeted PROTAC

    MS6105 is a selective LDH-targeted PROTAC that induces the degradation of LDHA and LDHB through the ubiquitin-proteasome system. This compound exhibits notable anticancer activity, making it a valuable tool for cancer research. Additionally, MS6105 features an alkyne group, facilitating copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules, enabling diverse applications in chemical biology and drug discovery.
  26. PD-L1-PROTAC Degrader

    PROTAC PD-L1 degrader-1 is a CRBN-based protein degrader targeting PD-L1, facilitating the selective degradation of the PD-L1 protein. This compound demonstrates potent PD-L1 degradation in 4T1 cells, with a DC50 value of 0.609 μM. It serves as a valuable tool for investigating therapeutic approaches in breast cancer research.
  27. PROTAC ERα Degrader

    ERD-3111 is an orally active PROTAC degrader targeting estrogen receptor alpha (ERα) with a reported DC50 of 0.5 nM. This compound effectively inhibits tumor growth in both wild-type MCF-7 xenograft models and in models harboring clinically relevant ESR1 mutations. ERD-3111 is a valuable tool for research focused on estrogen receptor-positive breast cancer, facilitating investigations into targeted degradation pathways and therapeutic strategies.
  28. PROTAC ER Degrader

    PROTAC ER Degrader-4 is a von Hippel-Lindau-based PROTAC that targets the estrogen receptor (ER). It demonstrates high potency, binding to ER with an IC50 of 0.8 nM, and effectively induces ER degradation in MCF-7 cells with an IC50 of 0.3 nM. This compound is valuable for research applications focused on hormone receptor signaling and targeted protein degradation.
  29. VHL-type PROTAC degrader

    PROTAC VHL-type degrader-1 is a VHL-type PROTAC degrader that facilitates the targeted degradation of the ATM protein. This compound enhances the efficacy of the ATR inhibitor AZD6738 through a synergistic mechanism, making it a valuable tool for investigating the interplay between ATM and ATR signaling pathways. It is applicable in research focusing on cancer therapeutics and cellular response to DNA damage.
  30. PROTACs

    AZ'6421 is a Protcolysis Targeting Chimera (PROTAC) designed to selectively degrade estrogen receptor alpha. It exhibits potent anti-tumor activity, effectively inhibiting uncontrolled cellular proliferation associated with malignancies. AZ'6421 is primarily utilized in cancer research, particularly for investigating breast cancer and its therapeutic strategies.
  31. AD4

    PCLAF Inhibitor

    AD4 is a proteolytic targeting chimera (PROTAC) designed to inhibit PCLAF. This compound effectively degrades PCLAF in RS4;11 cells with an IC50 of 0.6 nM, leading to the activation of the p21/Rb pathway and demonstrating anti-tumor effects. In vivo studies have shown that AD4 prolongs survival in RS4;11-transplanted NOD/SCID mice, highlighting its potential for cancer research applications.
  32. SMARCA2 PROTAC degrader

    YD54 is a PROTAC designed to induce degradation of the SMARCA2 protein, exhibiting a DC50 of 3.5 nM. This compound utilizes a targeted approach to promote the ubiquitination and proteasomal degradation of SMARCA2, making it a valuable tool for studying SMARCA2-dependent biological processes. YD54 is suitable for applications in cancer research and cellular signaling investigations, where modulation of SWI/SNF complex activity is critical.
  33. PARK7 Degrader

    JYQ-194 is a proteolysis-targeting chimera (PROTAC) designed to degrade human PARK7, a protein implicated in Parkinson's disease. This reagent serves as a valuable tool for investigating the underlying mechanisms of neurodegeneration and cancer biology. Its ability to selectively target and degrade PARK7 highlights its potential utility in therapeutic applications and biological research related to Parkinson's disease and other neurodegenerative conditions.
  34. PROTAC Axl Degrader

    PROTAC Axl Degrader 2 is a selective proteolysis-targeting chimera (PROTAC) that degrades Axl with an IC50 of 1.61 μM. This compound exhibits significant anti-proliferation and anti-migration activities in vitro. Additionally, PROTAC Axl Degrader 2 induces mehuosis, making it a valuable tool for studying Axl’s role in cancer progression and therapeutic resistance. Potential research applications include investigations into targeted degradation as a therapeutic strategy in oncology.
  35. STAT3 PROTAC Degrader

    PROTAC STAT3 degrader-3 (S3D1) targets the STAT3 protein through a PROTAC-mediated degradation mechanism. This compound exhibits potent anticancer activity by facilitating the ubiquitination and subsequent proteasomal degradation of STAT3, a key oncogenic transcription factor. It is primarily applied in research focused on cancer biology, particularly in studies investigating the therapeutic potential of targeting the STAT3 signaling pathway.
  36. Threonine Tyrosine Kinase PROTAC Degrader

    PROTAC TTK degrader-1 is a selective threonine tyrosine kinase (TTK) PROTAC degrader designed to induce target degradation. It demonstrates potent biological activity, with DC50 values of 1.7 nM and 5.8 nM in COLO-205 and HCT-116 cell lines, respectively. This compound exhibits significant anticancer efficacy in xenograft mouse models utilizing COLO-205 human colorectal cancer cells, making it a valuable tool for research in cancer therapeutics and targeted protein degradation.
  37. DDR1 PROTAC Degrader

    PROTAC DDR1 degrader-1 is a PROTAC-based degrader designed to selectively target the discoidin domain receptor 1 (DDR1) for proteasomal degradation. This compound utilizes a specific DDR1 inhibitor linked to an E3 ligase ligand, facilitating targeted protein degradation. It exhibits potential applications in elucidating DDR1's role in various cellular processes and disease states, providing valuable insights for therapeutic research.
  38. CRBN-type PROTAC

    WH-10417-099 is a CRBN-type PROTAC designed to induce the degradation of over 125 unique kinases through the ubiquitin biotinylation (E-STUB) mechanism. Its structure comprises a PI3Kγ ligand, a Thalidomide 4-fluoride E3 ubiquitin ligase ligand, and an Amino-PEG5-C2-acid linker. This compound is valuable for research into targeted protein degradation and multi-kinase signaling pathways, with potential applications in cancer and other diseases characterized by dysregulated kinase activity.
  39. PROTAC erf3a Degrader

    PROTAC erf3a Degrader-1 is a potent oral degrader designed to target the erf3a protein. This compound exhibits significant anti-proliferative activity against various cancer cell lines, including 22Rv1, making it a valuable tool in cancer research. PROTAC erf3a Degrader-1 is particularly relevant for studies focused on prostate, ovarian, liver, cervical, and breast cancers, as well as leukemia, facilitating the investigation of targeted protein degradation in these malignancies.
  40. USP7 PROTAC Degrader

    CST967 is a USP7 PROTAC degrader that facilitates targeted degradation of the USP7 protein through the ubiquitin-proteasome pathway. By modulating PROTAC concentration, researchers can significantly enhance the degradation rate of USP7, a key regulator in various cellular processes. This compound is valuable in cancer research for investigating the functional consequences of USP7 inhibition and exploring novel therapeutic strategies.
  41. SMARCA2 Degrader

    PROTAC SMARCA2 degrader-8 is a selective degrader targeting the SMARCA2 protein, exhibiting a DC50 of 28 nM in A375 cells. This compound facilitates the ubiquitination and subsequent proteasomal degradation of SMARCA2, thereby effectively reducing its cellular levels. It is particularly useful for studies investigating the role of SMARCA2 in various cancer types and for elucidating its mechanisms of action in cellular processes.
  42. CRBN Degrader

    ZXH-4-130 is a selective degrader of cereblon (CRBN) utilizing the CRBN-VHL mechanism. This compound effectively facilitates the degradation of target proteins through the ubiquitin-proteasome pathway, making it a valuable tool in studying protein homeostasis and degradation processes. Its applications extend to research in targeted protein degradation and the exploration of CRBN's role in various biological contexts.
  43. BRD4 PROTAC

    MS83 is a novel PROTAC that employs a KEAP1 ligand to target and degrade BRD4, along with its homologs BRD3 and BRD2. By harnessing the ubiquitin-proteasome system, MS83 facilitates targeted protein degradation, providing a powerful tool for dissecting the functional roles of BRD4 in cellular processes. This compound is particularly relevant for research on cancer and epigenetic regulation, offering insights into therapeutic strategies that leverage targeted protein degradation.
  44. BRD9 Degrader PROTAC

    PROTAC BRD9 Degrader-5 is a proteolysis-targeting chimera (PROTAC) that facilitates the targeted degradation of the bromodomain-containing protein BRD9. This compound employs the cellular ubiquitin-proteasome pathway to promote the selective elimination of BRD9, leading to the modulation of biological pathways associated with cancer and other diseases. It serves as a valuable tool for researchers investigating the role of BRD9 in various cellular processes and therapeutic interventions.
  45. PROTAC Pirin Degrader

    CCT367766 is a third-generation heterobifunctional PROTAC designed to target and degrade the pirin protein through the CRBN-DDB1 complex. This compound effectively reduces pirin expression at low concentrations, demonstrating an IC50 of 490 nM. It exhibits high binding affinities for recombinant pirin and CRBN, with Kd values of 55 nM and 120 nM, respectively. CCT367766 serves as a valuable chemical tool for probing the biological functions of pirin and advancing research in proteolysis-targeting chimeras.
  46. Photocaged-PROTAC

    phoBET1 is a photocaged-PROTAC targeting BRD4 for selective degradation. This compound harnesses light-activated control to induce the degradation of BRD4 protein, resulting in significant suppression of tumor growth. Its unique photocaging mechanism allows for spatial and temporal regulation of protein activity, making it a valuable tool for studying the role of BRD4 in cancer biology and therapeutic applications.
  47. Threonine Tyrosine Kinase PROTAC Degrader

    PROTAC TTK degrader-2 is a potent degrader that targets threonine tyrosine kinase (TTK), demonstrating DC50 values of 3.1 nM in COLO-205 cells and 12.4 nM in HCT-116 cells. This compound effectively induces target protein degradation and exhibits anticancer activity in a xenograft mouse model of human colorectal cancer derived from COLO-205 cells. It serves as a valuable tool for investigating TTK's role in cancer biology and may aid in the development of novel therapeutic strategies.
  48. SIAIS630121 Negative Control

    SIAIS630121-NC is a negative control compound designed for use alongside the NAMPT (nicotinamide phosphoribosyltransferase) PROTAC degrader SIAIS630121. This compound demonstrates no degradation activity on NAMPT, serving as a baseline reference for experimental validation. SIAIS630121-NC is essential for researchers studying the effects of NAMPT degradation and the role of PROTAC technology in targeted protein modulation.
  49. SMARCA2 Degrader degrader

    SMARCA2 degrader-20 is a potent PROTAC that targets the SMARCA2 protein for degradation, exhibiting a DC50 of less than 100 nM in A549 cells. This degrader is valuable for studying the functional consequences of SMARCA2 depletion in cancer biology and epigenetic regulation. Its high efficacy facilitates research into targeted protein degradation strategies and their therapeutic potential in oncology.
  50. PROTAC ER Degrader

    (Rac)-Vepdegestrant targets the estrogen receptor (ER) as a PROTAC (proteolysis-targeting chimera) degrader, effectively inducing the proteasomal degradation of estrogen receptors in breast cancer cells. This hetero-bifunctional compound enhances the interaction between ER-alpha and an E3 ligase complex, resulting in significant ubiquitylation. (Rac)-Vepdegestrant exhibits potent biological activity, showcasing a half-maximal degradation concentration (DC50) of approximately 2 nM in ER-positive breast cancer cell lines, making it a valuable tool for studying ER-related signaling pathways and potential therapeutic applications in breast cancer research.

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