PROTAC

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  1. Ligands for Target Protein for PROTAC Chemical

    PROTAC BRD4 ligand-2 is a specific ligand for the BRD4 protein, designed for use in PROTAC-mediated degradation strategies. This compound facilitates the targeted degradation of BRD4, a key regulator of transcription and associated with various cancers, by recruiting the E3 ubiquitin ligase. It is instrumental in research applications aimed at understanding BRD4's role in oncogenesis and therapeutic development in cancer treatments.
  2. BRD4 PROTAC Degrader

    PROTAC BRD4 Degrader-34 is a selective degrader that targets the bromodomain-containing protein 4 (BRD4) through a proteolysis-targeting chimera (PROTAC) mechanism. It induces the degradation of the BRD4-BD2 domain via the VHL E3 ubiquitin ligase system. This compound has significant potential for use in cancer research, enabling investigations into the therapeutic effects of targeting BRD4 in oncogenic pathways.
  3. SMARCA2/4 PROTAC degrader

    PROTAC SMARCA2/4 degrader-37 is a proteolysis-targeting chimera (PROTAC) that selectively degrades SMARCA2 and SMARCA4 proteins. It exhibits a potent inhibitory concentration (IC50) of ≤0.1 μM, highlighting its efficacy in disrupting these bromodomain-containing proteins. This reagent is suitable for applications in cancer research and therapeutic development, particularly in studies involving epigenetic modulation and chromatin remodeling.
  4. SMARCA2/4 Ligand

    SMARCA2/4-ligand-5 is a selective ligand targeting the SMARCA2 and SMARCA4 proteins, functioning as a crucial component in the PROTAC SMARCA2/4 degrader-37. This compound demonstrates potent biological activity, achieving an IC50 of ≤0.1 μM, making it suitable for applications in targeted protein degradation studies. Research utilizing SMARCA2/4-ligand-5 contributes to understanding the roles of these chromatin remodelers in various biological processes and cancer biology.
  5. RAF Molecular Glue

    NST-628 is a molecular glue targeting RAF within the MAPK signaling pathway. It disrupts RAF phosphorylation and MEK activation by preventing the formation of BRAF-CRAF and BRAF-ARAF heterodimers. NST-628 exhibits significant biological activity in inhibiting RAS- and RAF-driven cancers, particularly in tumors with mutant KRAS, NRAS, BRAF class II/III, and NF1 mutations. This compound is a valuable tool for research into targeted cancer therapies and understanding the RAS-MAPK pathway's role in oncogenesis.
  6. PROTAC BRAF-V600E Degrader

    PROTAC BRAF-V600E Degrader-2 is a highly selective degrader targeting the BRAF-V600E mutant, with dissociation constants (Kd) of 14.4 nM and 9.5 nM for BRAF and BRAF-V600E, respectively. This compound effectively induces degradation of the BRAF-V600E kinase domain without impacting wild-type BRAF. Its potent biological activity makes it a valuable tool for research applications focused on melanoma cell growth inhibition and the study of BRAF-related signaling pathways.
  7. Ligand of BRAF

    BRAF ligand-1 acts as a specific ligand for the BRAF protein, playing a crucial role in the regulation of cell signaling pathways associated with cell proliferation, survival, and differentiation. This compound is important for studying the BRAF signaling pathway and its implications in various cancers. Additionally, BRAF ligand-1 can be utilized in the synthesis of CST905, further enhancing its utility in biochemical research and drug discovery efforts targeting mutant BRAF.
  8. pan-KRAS PROTAC Degrader

    MCB-36 is a VHL-recruiting pan-KRAS PROTAC degrader that targets various KRAS mutants, including G12D, G12C, G12V, and wild-type forms, with an exceptionally high binding affinity (Kd ≈ 1 pM). This compound effectively lowers p-ERK levels, promoting apoptosis in KRAS-driven cancer cells while showing minimal impact on HRAS and NRAS protein levels. MCB-36 is particularly useful for investigating colorectal and lung cancers, as it demonstrates efficacy against KRASG12C inhibitor-resistant tumors and aids in remodeling the tumor immune microenvironment.
  9. Molecular Glue

    OPB-171775 is an orally active molecular glue that targets phosphodiesterase 3A (PDE3A) and schlafen family member 12 (SLFN12). This compound induces SLFN12-mediated RNase activity, leading to subsequent cell death. Additionally, OPB-171775 activates the GCN2 signaling pathway associated with SLFN12, showcasing its significant efficacy in combating gastrointestinal stromal tumors. Researchers can utilize OPB-171775 to explore pathways in cancer biology and investigate the therapeutic potential of molecular glues in tumor treatment.
  10. FKBP51 Degrader, VHL Binder

    SelDeg51 is a selective PROTAC degrader targeting FKBP51 with a Kd value of 18 nM and a maximum degradation efficacy (Dmax) of 90%. It facilitates the proteasomal degradation of FKBP51 through the formation of a ternary complex with FKBP51 and VHL, effectively reactivating glucocorticoid receptor signaling. SelDeg51 is particularly relevant for research in stress-related mental disorders, chronic pain, and obesity.
  11. FKBP12F36V PROTAC Degrader

    dTAGV-1 is a selective proteolysis-targeting chimera (PROTAC) degrader designed to target FKBP12F36V-tagged proteins. This compound effectively induces the degradation of FKBP12F36V-Nluc in vivo, making it a valuable tool for studying protein turnover and function. Its application is particularly relevant in cellular and molecular biology research, facilitating the investigation of protein interactions and therapeutic targets.
  12. PROTAC FKBP12 Degrader

    10-SLF is a PROTAC FKBP12 degrader that facilitates the formation of a ternary complex between FKBP12 and the mutant E3 ligase FBXW7-R465C. This compound promotes the FBXW7-R465C-mediated proteasomal degradation of FKBP12, selectively lowering FKBP12 levels in cells harboring the FBXW7-R465C mutation. 10-SLF is valuable for studying protein degradation pathways and the role of FKBP12 in various biological contexts.
  13. Nucleoprotein PROTAC Degrader

    KB03-SLF is an electrophilic PROTAC degrader targeting DCAF16 to facilitate the degradation of the nuclear protein FKBP12. This compound serves as a valuable tool in cancer research, enabling the investigation of protein homeostasis and degradation pathways. KB03-SLF’s unique structure incorporates specific ligands that enhance its efficacy as a degradative agent, making it a significant asset for studies focused on targeted protein elimination.
  14. FKBP12 PROTAC Degrader

    RAFKBP12 is a PROTAC degrader that specifically targets FKBP12, utilizing the CAP-TAC strategy to facilitate proteasome-dependent degradation. This compound operates independently of E3 ubiquitin ligases and protein ubiquitination, demonstrating its innovative mechanism of action. RAFKBP12 serves as a valuable tool for research in protein degradation pathways and therapeutic applications related to FKBP12 modulation.
  15. LRRK2 PROTAC Degrader

    PROTAC LRRK2 Degrader-1 is a targeted protein degrader that selectively engages leucine-rich repeat kinase 2 (LRRK2), exhibiting an IC50 value of less than 10 nM. This compound is designed for the study of LRRK2-mediated pathways and offers significant potential for advancing research on Parkinson's disease. Its ability to induce targeted degradation makes it a valuable tool for investigating therapeutic strategies in neurodegenerative disorders associated with LRRK2 dysregulation.
  16. LRRK2 PROTAC Degrader

    ROTAC LRRK2 degrader-1 is a potent PROTAC degrader targeting LRRK2, a protein associated with neurodegenerative diseases. This compound facilitates the targeted degradation of LRRK2, which is implicated in the pathogenesis of Parkinson’s Disease. ROTAC LRRK2 degrader-1 can be utilized in research to investigate LRRK2-related biological pathways and therapeutic interventions for Parkinson’s Disease and other associated disorders.
  17. LRRK2 PROTAC Degrader

    PROTAC LRRK2 Degrader-2 is designed to target LRRK2 through a PROTAC mechanism, exhibiting a DC50 of 0.14 nM. This compound effectively recruits LRRK2 or its mutants to the cereblon E3 ubiquitin ligase, facilitating targeted ubiquitination and subsequent proteasomal degradation of LRRK2. It serves as a valuable tool for research focused on Parkinson's disease and the study of LRRK2-related pathways.
  18. PROTAC Linkers

    Fmoc-NH-PEG5-CH2COOH is a cleavable linker specifically designed for use in antibody-drug conjugates (ADCs) and as a PEG-based link in the synthesis of PROTACs. This compound facilitates the efficient conjugation of therapeutic agents to antibodies, enhancing targeted delivery. Its unique structure allows for controlled release, making it valuable in the development of innovative therapeutic strategies in drug discovery and bioconjugation research.
  19. ADC/PROTAC Linker

    DBCO-NHCO-PEG4-NH-Boc is a versatile PROTAC linker featuring a cleavable structure designed for the synthesis of PROTACs and antibody-drug conjugates (ADCs). This compound utilizes a DBCO moiety, enabling efficient strain-promoted alkyne-azide cycloaddition (SPAAC) with azide-containing molecules. Its PEG4 spacer enhances solubility and stability, making it suitable for various biological applications in drug development and therapeutic research.
  20. ADC/PROTAC Linker

    DBCO-NHCO-PEG4-amine is a PEG-based linker designed for use in antibody-drug conjugates (ADCs) and PROTACs. This cleavable linker facilitates the conjugation of payloads such as MMAE to antibodies, enhancing targeted delivery to cancer cells. It has demonstrated compelling biological activities, with EC50 values of 280 nM and 22 nM for DBCO-VCpAB MMAE and DBCO-TRX MMAE, respectively, in SKBR3 cells, making it a valuable tool for researchers investigating targeted therapies.
  21. ADC/PROTAC Linker

    Tr-PEG3-OH is a non-cleavable linker comprised of a three-unit polyethylene glycol (PEG) chain, designed for use in the synthesis of antibody-drug conjugates (ADCs). This compound enhances the solubility and stability of ADCs, facilitating targeted delivery of cytotoxic agents to specific cells. Its applications extend to PROTAC (proteolysis-targeting chimera) technology, enabling the development of innovative therapies that harness targeted protein degradation.
  22. ADC/PROTAC Linker

    Propargyl-PEG7-acid is a PEG-based linker designed for use in antibody-drug conjugates (ADCs) and proteolysis-targeting chimeras (PROTACs). It features a propargylic group that facilitates copper-catalyzed azide-alkyne cycloaddition (CuAAc), enabling effective conjugation to azide-containing molecules. This compound serves as a cleavable linker, providing versatility in drug delivery systems and targeted therapy research. Propargyl-PEG7-acid is essential for studies focusing on the development of innovative therapeutic modalities through advanced chemical synthesis techniques.
  23. PROTAC Linkers

    DBCO-N-bis(PEG4-NHS ester) is a bifunctional polyethylene glycol (PEG) linker featuring two NHS ester groups and a dibenzocyclooctyne (DBCO) moiety. This reagent facilitates protein modification and labeling, enhancing bioconjugation applications. As a click chemistry tool, DBCO-N-bis(PEG4-NHS ester) enables efficient strain-promoted alkyne-azide cycloaddition (SPAAC) with azide-containing molecules, making it valuable for constructing PROTAC molecules and other bioorthogonal conjugates in various biochemical research settings.
  24. ADC/PROTAC Linker

    Azido-PEG4-Val-Cit-PAB-OH is a cleavable polyethylene glycol (PEG) linker designed for use in antibody-drug conjugates (ADCs) and proteolysis-targeting chimeras (PROTACs). This compound features an azide group, enabling it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc) with alkyne-containing molecules, as well as strain-promoted alkyne-azide cycloaddition (SPAAC) with DBCO or BCN moieties. Its versatility as a click chemistry reagent supports diverse applications in chemical biology and drug development.
  25. PROTAC Linkers

    m-PEG11-acid is a non-cleavable linker composed of 11 ethylene glycol units, functioning as a versatile agent in the synthesis of antibody-drug conjugates (ADCs) and PROTACs. This polyethylene glycol (PEG)-based linker enhances the solubility and pharmacokinetics of the conjugates while facilitating targeted degradation of proteins in research applications. m-PEG11-acid is crucial for investigating the mechanisms of protein regulation and therapeutic strategies in drug discovery.
  26. ADC/PROTAC Linker

    m-PEG4-MS is a polyethylene glycol (PEG)-based linker designed for use in the synthesis of PROTACs and antibody-drug conjugates (ADCs). This cleavable linker facilitates the precise delivery of therapeutic agents, enhancing the stability and efficacy of the resulting compounds. Its application in PROTAC development and ADC formulation supports research into targeted protein degradation and innovative cancer therapies.
  27. ADC/PROTAC Linker

    m-PEG7-Amine is a polyethylene glycol (PEG)-based linker designed for use in PROTAC (Proteolysis Targeting Chimeras) and antibody-drug conjugate (ADC) synthesis. This cleavable linker facilitates the targeted degradation of specific proteins, enhancing the efficacy of PROTACs. Its versatile application makes it an essential component in developing therapeutic modalities aimed at selective protein modulation and cancer treatment.
  28. PROTAC Linkers

    m-PEG10-alcohol is a non-cleavable linker comprised of a decaethylene glycol unit, primarily used in the design of antibody-drug conjugates (ADCs). This PEG-based compound serves as a versatile PROTAC linker, facilitating the development of proteolysis-targeting chimeras. Its structure enhances solubility and stability, making it suitable for various chemical biology applications, including targeted protein degradation studies.
  29. PROTAC Linkers

    (2R,4R)-4-Hydroxypyrrolidine-2-carboxylic acid hydrochloride functions as a non-cleavable linker in the development of antibody-drug conjugates (ADCs). Furthermore, it serves as an alkyl chain-based PROTAC linker, facilitating the synthesis of PROTACs. This compound plays a crucial role in advancing targeted protein degradation research, contributing to the exploration of innovative therapeutic strategies.
  30. PROTAC Linker

    PC Alkyne-PEG4-NHS ester is a cleavable linker designed for use in the synthesis of antibody-drug conjugates (ADCs). Functioning as a PROTAC linker, this reagent features an alkyne group and participates in copper-catalyzed azide-alkyne cycloaddition (CuAAc) reactions. Its unique structure enhances the specificity and efficiency of conjugating azide-containing molecules, making it valuable for various chemical biology applications, including targeted drug delivery and proteolysis targeting chimera (PROTAC) development.
  31. PROTAC Linker

    TCO-PEG4-DBCO is a versatile PROTAC linker known for its ability to facilitate the synthesis of proteolysis-targeting chimeras (PROTACs). This compound features a DBCO moiety that enables strain-promoted alkyne-azide cycloaddition (SPAAC) with azide-containing compounds, while the TCO component allows for inverse electron demand Diels-Alder (iEDDA) reactions with tetrazine derivatives. TCO-PEG4-DBCO finds applications in the development of antibody-drug conjugates (ADCs), enhancing the precision and efficacy of targeted therapeutics. Its unique chemical properties make it a valuable tool for researchers in chemical biology and drug development.
  32. ADC/PROTAC Linker

    Propargyl-PEG8-bromide is a PEG-based linker designed for use in antibody-drug conjugates (ADCs) and PROTAC synthesis. This non-cleavable linker includes an alkyne group, enabling its application in click chemistry through copper-catalyzed azide-alkyne cycloaddition (CuAAc). Its versatility makes it a valuable tool for researchers in the development of targeted therapeutics and for probing protein degradation mechanisms.
  33. PROTAC Linkers

    m-PEG10-acid is a polyethylene glycol (PEG) linker designed for use in the synthesis of antibody-drug conjugates (ADCs) and PROTACs (Proteolysis Targeting Chimeras). This non-cleavable 10-unit PEG linker enhances solubility and stability, facilitating effective delivery of therapeutic agents to targeted cells. The compound is instrumental in chemical biology applications, aiding in the development of novel targeted therapies and research into protein degradation mechanisms.
  34. PROTAC Linkers

    N-Bromoacetyl-β-alanine is a versatile PROTAC linker that functions through targeted protein degradation pathways. This compound facilitates the synthesis of PROTACs, enabling the development of novel therapeutic strategies. Additionally, N-Bromoacetyl-β-alanine serves as a cleavable linker for antibody-drug conjugates (ADCs), enhancing the delivery of cytotoxic agents to specific cancer cells. Its utility in these applications makes it a valuable tool in chemical biology research.
  35. PROTAC Linker

    β-D-tetraacetylgalactopyranoside-PEG1-N3 serves as a cleavable linker in PROTAC (proteolysis-targeting chimera) research, facilitating the synthesis of antibody-drug conjugates (ADCs). This compound features an azide group that allows for click chemistry applications, including copper-catalyzed azide-alkyne cycloaddition (CuAAc) with alkyne-containing molecules. Additionally, it is capable of undergoing strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with partners containing DBCO or BCN moieties, making it a versatile tool for bioconjugation and targeted drug delivery studies.
  36. ADC/PROTAC Linker

    m-PEG8-MS is a polyethylene glycol (PEG)-based linker designed for use in antibody-drug conjugates (ADCs) and proteolysis-targeting chimeras (PROTACs). This cleavable linker facilitates the effective synthesis of ADCs, enhancing drug delivery specificity and potency. Its versatile applications in chemical biology allow for targeted degradation of selected proteins, making it a valuable tool in therapeutic development and research.
  37. ADC/PROTAC Linker

    Propargyl-PEG1-SS-PEG1-C2-Boc is a versatile alkyl/ether-based linker with applications in PROTAC and antibody-drug conjugate (ADC) synthesis. This cleavable linker features an alkyne group, enabling its use in click chemistry via copper-catalyzed azide-alkyne cycloaddition (CuAAc). Propargyl-PEG1-SS-PEG1-C2-Boc is instrumental in the development of targeted therapeutic strategies, making it valuable for researchers in drug design and bioconjugation studies.
  38. PROTAC Linker

    Tr-PEG8-OH is a non-cleavable linker composed of an 8 unit polyethylene glycol (PEG) chain, primarily utilized in the synthesis of PROTACs (proteolysis-targeting chimeras) and antibody-drug conjugates (ADCs). This PEG-based linker facilitates the development of optimized bioconjugates, enhancing their pharmacokinetic profiles and therapeutic efficacy. Tr-PEG8-OH is particularly valuable for research applications focusing on targeted protein degradation and drug delivery systems.
  39. ADC/PROTAC Linker

    Propargyl-PEG4-thiol is a PEG-based linker specifically designed for use in the synthesis of PROTACs and non-cleavable antibody-drug conjugates (ADCs). This compound features an alkyne functional group that participates in copper-catalyzed azide-alkyne cycloaddition (CuAAc), facilitating precise conjugation with azide-containing molecules. Propargyl-PEG4-thiol is essential for advancing research in targeted protein degradation and therapeutic antibody development.
  40. ADC/PROTAC Linker

    m-PEG7-MS is a polyethylene glycol (PEG)-based linker designed for use in the synthesis of PROTACs and antibody-drug conjugates (ADCs). This cleavable linker facilitates the development of targeted therapeutics by enabling controlled release of active compounds. Its versatile application supports research in targeted protein degradation and drug delivery systems, making it an essential reagent for advancing science in cancer therapy and other diseases.
  41. ADC/PROTAC Linker

    DBCO-NHCO-PEG4-NHS ester is a versatile linker designed for use in the synthesis of PROTACs and antibody-drug conjugates (ADCs). This PEG/alkyl/ether-based compound features a DBCO moiety that facilitates strain-promoted alkyne-azide cycloaddition (SPAAC) with azide-containing molecules. Its cleavable nature enhances the functionality and targeting capabilities of therapeutic agents, making it essential for researchers involved in drug development and bioconjugation applications.
  42. ADC/PROTAC Linker

    N-Boc-N-bis(PEG4-OH) is a PEG-based linker designed for use in PROTAC (proteolysis-targeting chimera) synthesis. This cleavable linker also serves as a versatile component for the development of antibody-drug conjugates (ADCs). Due to its unique structure, it facilitates targeted drug delivery and enhances the efficacy of therapeutic agents in various biological applications.
  43. PROTAC Linkers

    Bis-PEG7-acid is a polyethylene glycol (PEG) based linker specifically designed for use in the synthesis of PROTACs (proteolysis-targeting chimeras). This compound enhances the solubility and stability of the PROTAC molecules, facilitating targeted protein degradation. Its application in chemical biology supports research focused on developing novel therapeutics through targeted ubiquitination pathways.
  44. ADC/PROTAC Linker

    Propargyl-PEG9-bromide is a PEG-based linker utilized in the synthesis of PROTACs and antibody-drug conjugates (ADCs). This non-cleavable linker facilitates the targeted delivery of therapeutics through its unique click chemistry capabilities, featuring an alkyne group suitable for copper-catalyzed azide-alkyne cycloaddition (CuAAc). Its applications extend to enhancing drug efficacy and specificity in chemical biology and therapeutic development.
  45. PROTAC Linkers

    m-PEG4-Boc is a cleavable polyethylene glycol (PEG) linker with four ethylene glycol units, designed for use in the synthesis of antibody-drug conjugates (ADCs) and Proteolysis Targeting Chimeras (PROTACs). This versatile linker facilitates the development of ADCs by enabling site-specific conjugation, while also serving as a crucial component in PROTAC design for targeted protein degradation. Its functional properties contribute to the effectiveness and stability of various bioconjugates in chemical biology research.
  46. PROTAC linker

    Boc-gly-PEG3-endo-BCN is a cleavable PEG-based linker designed for targeted protein degradation applications through PROTAC technology. Its biocompatible structure facilitates the synthesis of antibody-drug conjugates (ADCs) by serving as a versatile linker. The presence of a bicyclo[6.1.0]nonyne (BCN) group allows for efficient strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with azide-containing molecules, making it a valuable reagent for click chemistry in biological research.
  47. ADC/PROTAC Linker

    m-PEG5-MS is a PEG-based linker designed for antibody-drug conjugates (ADCs) and proteolysis-targeting chimeras (PROTACs). This cleavable linker facilitates the synthesis of PROTACs, enabling targeted degradation of specific proteins. Its key applications include drug development and cellular regulation studies, making it a versatile tool in therapeutic research and protein modulation.
  48. PROTAC Linker

    Amino-PEG11-OH is a non-cleavable linker composed of an 11-unit polyethylene glycol (PEG) moiety designed for use in antibody-drug conjugates (ADCs) and PROTAC (Proteolysis Targeting Chimera) synthesis. This PEG-based linker facilitates the conjugation of drugs to antibodies, enhancing therapeutic efficacy while maintaining stability. Additionally, it serves as an effective component in the development of PROTACs, enabling targeted protein degradation for advanced molecular research applications.
  49. ADC/PROTAC Linker

    Propargyl-PEG7-NHS ester is a PEG-based linker designed for use in the synthesis of PROTACs and antibody-drug conjugates (ADCs). This cleavable linker features an alkyne group, facilitating copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules. Its versatility and efficiency make it a valuable tool in the development of targeted therapeutics and bioconjugates for cancer research and drug delivery applications.
  50. ADC/PROTAC Linker

    N-Boc-N-bis(PEG2-OH) is a PEG-based linker designed for use in antibody-drug conjugates (ADCs) and PROTAC synthesis. This cleavable linker facilitates the precise attachment of therapeutic agents to antibodies, enhancing targeted drug delivery while minimizing off-target effects. Its structure allows for efficient conjugation and release of the active component, making it suitable for a variety of applications in drug development and molecular biology research.

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