PROTAC

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  1. PROTAC HPK1 Degrader

    DD205-291 is an orally active PROTAC HPK1 degrader that exhibits a DC50 value of 5.3 nM. Its primary mechanism involves the targeted degradation of HPK1, leading to the inhibition of SLP-76 phosphorylation. This modulation subsequently results in the enhanced expression of key cytokines such as IL-2 and IFN-γ, making DD205-291 a valuable reagent for studies in immune signaling and related therapeutic applications.
  2. Ligands for Target Protein for PROTAC

    PD0325901-O-C2-dioxolane is a derivative of the MEK inhibitor PD0325901, designed as a ligand for targeted protein degradation in conjunction with VHL or CRBN E3 ligases. This compound facilitates the synthesis of MEK1/2 degraders, enabling the selective degradation of MEK proteins in experimental studies. Its application in research provides critical insights into MEK-related signaling pathways and their role in various diseases, particularly in cancer biology.
  3. MEK1/2 PROTAC Degrader

    MS910 is a potent and selective PROTAC degrader targeting MEK1 and MEK2 kinases. It demonstrates effective degradation of MEK1 and MEK2 in various cancer cell lines, with reported DC50 values of 118 nM for MEK1 and 55 nM for MEK2 in HT-29 cells, and 94 nM for MEK1 and 38 nM for MEK2 in SK-MEL-28 cells. MS910 is primarily utilized in cancer research to explore the therapeutic potential of targeted protein degradation.
  4. Mixed Lineage Kinase PROTAC Degrader

    PROTAC MLKL Degrader-1 selectively targets and degrades MLKL, achieving a maximum efficacy (Dmax) greater than 90%. This compound incorporates modified CRBN ligands and linker components, functioning effectively in cellular models. PROTAC MLKL Degrader-1 effectively inhibits cell death in a TNF-α, Smac, and zVAD (TSZ) model of necroptosis, making it a valuable tool for investigating necroptosis pathways and their implications in various diseases.
  5. Ligand for Target Protein for PROTAC

    PROTAC SOS1 ligand 1 is a high-affinity ligand for the SOS1 protein, facilitating targeted protein degradation through PROTAC technology. This compound is instrumental in the development of therapeutic strategies by enabling the selective modulation of SOS1, which plays a pivotal role in various oncogenic signaling pathways. Researchers can utilize this reagent in studies focused on cancer biology and drug discovery, particularly in exploring novel approaches to target and degrade specific proteins associated with tumor progression.
  6. PROTAC Linker

    (2E,9Z)-Octadeca-2,9-dienoic acid serves as a PROTAC linker in chemical research applications. This polyunsaturated fatty acid plays a critical role in lipoxygenase-dependent metabolic processes, facilitating the study of enzyme-modulating pathways. Its unique structure enables the development of targeted protein degradation strategies in cellular systems.
  7. MALT1 PROTAC Degrader

    PROTAC MALT1 Degrader-1 is a selective degrader targeting MALT1 through the use of the PROTAC (proteolysis targeting chimera) technology. This compound facilitates the ubiquitination and subsequent proteasomal degradation of MALT1, making it a valuable tool for studies focused on lymphoma and related malignancies. Its mechanism of action enables the investigation of MALT1's role in cellular processes and therapeutic strategies for lymphoma treatment.
  8. PROTAC Linkers

    m-PEG-NHS ester (MW 5000) is a PEGylated linker that facilitates the synthesis of PROTACs (proteolysis-targeting chimeras). This compound features an N-hydroxysuccinimide (NHS) functional group, enabling efficient coupling to amine-containing substrates. Its hydrophilic nature enhances solubility and improves pharmacokinetic properties, making it an essential tool for researchers in targeted protein degradation and therapeutic development.
  9. E3 Ligase Ligand-Linker Conjugate

    (S,R,S)-AHPC-C5-COOH is an E3 ligase ligand-linker conjugate designed for the construction of PROTACs. It incorporates the VH032 VHL-based ligand, which is a selective and potent inhibitor of the VHL/HIF-1α interaction with a Kd of 185 nM. This compound is valuable for investigating models of anemia and ischemic diseases, providing a tool for targeted protein degradation research.
  10. IDO1 PROTAC Degrader

    NU227326 is a potent IDO1 PROTAC degrader designed to penetrate the blood-brain barrier, exhibiting a DC50 of 4.5 nM in HiBiT degradation assays. It effectively degrades IDO1 in human glioblastoma cell lines U87 and GBM43, with DC50 values of 7.1 nM and 11.8 nM, respectively, as demonstrated in Western blot assays. This compound is valuable for research into various malignancies, including glioblastoma, prostate cancer, triple-negative breast cancer, pancreatic cancer, and ovarian cancer.
  11. PROTAC IDO1 Degrader

    NU223612 is a selective PROTAC designed to target and degrade indoleamine 2,3-dioxygenase 1 (IDO1) through CRBN-mediated proteasomal degradation, exhibiting a Kd of 640 nM. With a binding affinity for CRBN of 290 nM, NU223612 effectively reduces IDO1 protein levels, making it a valuable tool in the study of immune modulation and tumor microenvironments. Additionally, NU223612 demonstrates the ability to cross the blood-brain barrier, enhancing its potential utility in neurobiological research.
  12. PROTAC Linkers

    DSPE-PEG-Biotin, MW 2000 is a polyethylene glycol (PEG) based linker designed for use in the synthesis of proteolysis-targeting chimeras (PROTACs). This compound facilitates the conjugation of biotin to target proteins, enhancing their recognition and degradation by the cellular proteasome. Its application in PROTAC technology supports the development of novel therapeutics by enabling targeted protein modulation in cellular research.
  13. PROTAC linker

    DSPE-PEG8-Mal is a PEG-based linker designed for use in PROTAC (proteolysis-targeting chimera) synthesis. This compound facilitates the development of PROTACs by enhancing their solubility and stability. Its primary mechanism involves forming a covalent bond with target proteins, thus enabling targeted degradation. DSPE-PEG8-Mal is essential for researchers investigating novel therapeutic strategies via targeted protein degradation.
  14. PROTAC TG2 degrader

    PROTAC TG2 degrader-1 is a von Hippel-Lindau (VHL)-based PROTAC designed to specifically target tissue transglutaminase (TG2) with a dissociation constant (KD) of 68.9 μM. This compound effectively induces the degradation of TG2 in ovarian cancer cells through a proteasome-dependent mechanism. It serves as a valuable tool for research investigating the role of TG2 in cancer biology and potential therapeutic applications.
  15. sEH PROTAC Degrader

    PROTAC sEH-degrader-3 is a selective sEH PROTAC degrader that specifically targets soluble epoxide hydrolase (sEH) in the cytosol, sparing its activity in peroxisomes. This compound induces degradation of sEH via a CRBN-mediated lysosomal pathway, exhibiting an IC50 of 0.8 nM against human sEH. PROTAC sEH-degrader-3 is valuable for research focusing on endoplasmic reticulum stress, inflammation, and metabolic diseases, offering insights into therapeutic strategies targeting these pathways.
  16. PROTAC Linker

    8-Hydroxyoctanoic acid is a versatile PROTAC linker that facilitates the synthesis of proteolysis-targeting chimeras (PROTACs). This compound enhances the selective degradation of target proteins through its ability to connect ligand and E3 ligase components. It is a valuable tool for researchers in drug discovery and cellular biology, enabling studies on targeted protein degradation mechanisms and therapeutic applications.
  17. PROTAC Linker

    Boc-NH-bicyclo[1.1.1]pentane-C-NH2 functions as a PROTAC linker, facilitating the development of proteolysis-targeting chimeras (PROTACs). This compound is essential for linking a target protein to an E3 ligase, thereby promoting ubiquitination and subsequent degradation of the target protein. It is valuable in various research applications, including targeted protein degradation studies and exploring protein homeostasis mechanisms.
  18. PROTAC Linker

    4-(2-Bromoethyl)phenol is a versatile PROTAC linker utilized in the synthesis of proteolysis-targeting chimeras (PROTACs). This compound facilitates the conjugation of target binding moieties to E3 ligase ligands, enabling targeted protein degradation. It is instrumental in the development of innovative therapeutic strategies through modulation of cellular pathways in various biological research applications.
  19. PROTAC Linker

    4-Bromo-1-trimethylsilyl-1-butyne serves as a versatile linker for the development of PROTAC (proteolysis-targeting chimera) molecules. Its unique structural features facilitate the conjugation of target ligands, thereby enabling the selective degradation of proteins through the ubiquitin-proteasome system. This compound is critical for advancing research in targeted protein degradation and enhancing therapeutic strategies in cancer and other diseases.
  20. PROTAC Linker

    N-Fmoc-8-aminooctanoic acid serves as a versatile PROTAC linker, facilitating the synthesis of proteolysis-targeting chimeras (PROTACs). This compound features an alkane chain that includes a terminal Fmoc-protected amine and a carboxylic acid group. The Fmoc group can be removed under basic conditions to yield a free amine amenable for further modifications. Additionally, the carboxylic acid can react with primary amines in the presence of coupling agents, such as EDC or HATU, to establish stable amide bonds, thus enhancing the structural diversity of PROTAC molecules for targeted protein degradation studies.
  21. PROTAC Linkers

    Boc-NH-PEG2-C2-NHS ester is an alkyl/ether-based PROTAC linker that facilitates the synthesis of proteolysis-targeting chimeras (PROTACs). This compound enables the conjugation of target proteins with E3 ligases, thereby promoting targeted degradation pathways. Its application in chemical biology allows for the development of innovative therapeutic strategies through the modulation of protein levels within cells.
  22. PROTAC Linker

    Azido-PEG6-azide is a PEG-based linker designed for use in the synthesis of PROTACs (proteolysis-targeting chimeras). Featuring an azide functional group, it facilitates click chemistry through copper-catalyzed azide-alkyne cycloaddition (CuAAc) with alkyne-containing molecules. Additionally, it can participate in strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with dibenzocyclooctyne (DBCO) or bicyclononyne (BCN) groups, making it a versatile tool for targeted protein degradation studies.
  23. PROTAC Linkers

    Bis-PEG12-acid is a polyethylene glycol (PEG)-based linker designed for use in the synthesis of proteolysis-targeting chimeras (PROTACs). This compound enhances the solubility and stability of PROTACs, facilitating the targeted degradation of specific proteins within cells. Bis-PEG12-acid is ideal for research applications focused on proteostasis, targeted therapy development, and the study of protein function through degradation mechanisms.
  24. PROTAC Linkers

    m-PEG7-alcohol is a polyethylene glycol (PEG)-based PROTAC linker designed for the synthesis of proteolysis targeting chimeras (PROTACs). This compound facilitates the development of innovative therapeutic strategies by linking target proteins to E3 ligases, enhancing protein degradation. Its unique structure offers improved solubility and biocompatibility, making it suitable for various chemical biology applications. This linker is essential for researchers aiming to manipulate protein levels within cellular environments.
  25. PROTAC Linkers

    HO-PEG11-OH is a PEG-based linker designed for use in the synthesis of PROTACs (proteolysis-targeting chimeras). This compound facilitates the effective conjugation of target proteins to E3 ligases, enhancing the recruitment and degradation of specific proteins via the ubiquitin-proteasome pathway. HO-PEG11-OH is valuable in research applications focusing on targeted protein degradation, therapeutic development, and cellular signaling studies.
  26. PROTAC Linker

    Mal-PEG8-acid is a PEG-based linker designed for use in PROTAC (Proteolysis Targeting Chimera) synthesis, facilitating targeted protein degradation. This compound enhances the solubility and stability of PROTACs while promoting efficient cellular uptake. It is a valuable tool in chemical biology for studying protein interactions and developing therapeutic agents targeting specific proteins for degradation.
  27. PROTAC Linkers

    Amino-PEG6-amine is a polyethylene glycol (PEG) compound featuring a six-unit linker that serves as an essential component in the synthesis of PROTACs (Proteolysis Targeting Chimeras). Its primary mechanism involves facilitating the conjugation of target proteins to E3 ligases, enabling selective degradation pathways. This reagent is crucial for advancing research in targeted protein degradation and protein engineering applications.
  28. PROTAC Linker

    Azide-PEG4-Tos is a PEG-based PROTAC linker known for facilitating the synthesis of proteolysis-targeting chimeras (PROTACs). Featuring an azide functional group, it participates in copper-catalyzed azide-alkyne cycloaddition (CuAAc) reactions with alkyne-containing compounds, as well as strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with DBCO or BCN derivatives. This compound is valuable for researchers focusing on targeted protein degradation and drug development through the innovative PROTAC technology.
  29. PROTAC Linkers

    Biotin-PEG4-SH is a polyethylene glycol (PEG)-based linker designed for the synthesis of PROTAC (Proteolysis Targeting Chimeras) molecules. This compound facilitates the conjugation of biotin to target proteins, enabling targeted degradation through the ubiquitin-proteasome pathway. Its primary applications include the development of novel PROTACs for targeted protein modulation in various biological studies and therapeutic investigations.
  30. PROTAC Linker

    Biotin-PEG-Biotin is a polyethylene glycol (PEG) linkage compound designed for use in the synthesis of PROTACs (Proteolysis Targeting Chimeras). This bifunctional linker enhances the solubility and bioavailability of target proteins, facilitating efficient degradation through the ubiquitin-proteasome system. Its primary applications include the development of novel therapeutic agents for targeted protein degradation in various diseases, including cancer and neurodegenerative disorders.
  31. PROTAC Linker

    Thiol-PEG3-acid is a polyethylene glycol (PEG)-based linker designed for use in the synthesis of PROTACs (proteolysis targeting chimeras). Its thiol moiety provides a reactive site for conjugation, facilitating the development of novel therapeutics that leverage targeted degradation mechanisms. This compound is essential for enhancing the solubility and stability of PROTACs, making it a valuable tool in chemical biology and drug discovery applications.
  32. PROTAC Linker

    Amino-PEG12-alcohol is a polyethylene glycol (PEG)-based linker designed for use in the synthesis of Proteolysis Targeting Chimeras (PROTACs). It facilitates the selective degradation of target proteins by linking an E3 ligase ligand with a target protein binder. This reagent is valuable for research applications in targeted protein degradation and developing novel therapeutic strategies.
  33. PROTAC Linker

    m-PEG5-acid is a polyethylene glycol-based linker designed for use in the synthesis of PROTACs (Proteolysis Targeting Chimeras). This compound facilitates the conjugation of target proteins to E3 ligases, enhancing the formation of PROTACs and promoting targeted protein degradation. m-PEG5-acid is instrumental in advancing research in protein modulation and therapeutic development.
  34. PROTAC Linker

    Diethylene glycol bis(p-toluenesulfonate) is a PEG-based linker designed for use in the synthesis of PROTACs (Proteolysis Targeting Chimeras). This compound facilitates the targeted degradation of specific proteins by bridging an E3 ligase and a protein of interest, enabling the selective modulation of cellular pathways. Its application is particularly relevant in drug discovery and development aimed at treating diseases associated with protein dysregulation.
  35. PROTAC Linkers

    Boc-NH-PEG6-CH2COOH is a PEG-based linker designed for use in the synthesis of PROTACs (Proteolysis Targeting Chimeras). This compound facilitates the conjugation of target proteins and E3 ligases, thereby enabling targeted protein degradation. It is essential for researchers developing PROTACs to study protein function and regulation in various biological contexts.
  36. PROTAC Linker

    tert-Butyl 5-bromoisoindoline-2-carboxylate serves as a PROTAC linker, facilitating targeted protein degradation mechanisms. This compound is instrumental in synthesizing various PROTACs, including the HSD17B13 degrader 1, which enables the modulation of protein levels within biological systems. Its structural properties make it a valuable tool in research applications focused on targeted therapy development and protein regulation studies.
  37. PROTAC Linker

    t-Boc-N-amido-PEG5-acetic acid is a polyethylene glycol (PEG)-based linker designed for use in the synthesis of PROTACs (proteolysis-targeting chimeras). This compound features a terminal carboxylic acid, facilitating conjugation with targeting ligands and degradation tags. It exhibits key biological activity in promoting targeted protein degradation, making it a valuable tool in drug discovery and development research applications.
  38. PROTAC Linker

    3-Iodopropan-1-ol is a PROTAC linker characterized by its role in the development of proteolysis-targeting chimeras (PROTACs). This compound facilitates the conjugation of target proteins to E3 ligase, promoting their ubiquitination and subsequent degradation. It is a valuable tool in research applications aimed at exploring targeted protein degradation and elucidating cellular pathways.
  39. PROTAC Linker

    m-PEG7-thiol is a polyethylene glycol (PEG)-based linker designed for use in the synthesis of PROTACs (proteolysis-targeting chimeras). This compound exhibits excellent solubility and flexibility, facilitating the efficient conjugation of target proteins with E3 ligases. It serves as a crucial component in the development of novel therapeutic modalities that harness the ubiquitin-proteasome system for targeted protein degradation in various research applications.
  40. PROTAC Linker

    Tetrazine-Ph-NHCO-C3-NHS ester serves as a PEG-based PROTAC linker, facilitating the synthesis of Proteolysis Targeting Chimeras (PROTACs). This compound features a Tetrazine group that enables a selective inverse electron demand Diels-Alder reaction (iEDDA) with TCO-containing molecules. It is instrumental in developing targeted protein degradation strategies in chemical research, enhancing the precision of therapeutic interventions.
  41. PROTAC Linker

    Fmoc-NH-PEG8-NHS ester is a polyethylene glycol (PEG) linker designed for use in PROTAC (PROteolysis TArgeting Chimeras) synthesis. This compound facilitates the conjugation of target proteins to E3 ligases, enhancing targeted protein degradation. Its long PEG chain improves solubility and bioavailability, making it a valuable tool in chemical biology and drug discovery applications focused on modulating protein levels within cells.
  42. PROTAC Linker

    Amino-PEG2-C2-hydrazide-Boc is a PEG-based linker designed for use in the synthesis of PROTACs (Proteolysis Targeting Chimeras). This compound facilitates the efficient conjugation of target proteins to E3 ligases, enhancing the degradation of specific proteins through the ubiquitin-proteasome pathway. Its versatile structure allows for a variety of applications in chemical biology and drug discovery, particularly in targeted protein degradation research.
  43. PROTAC Linker

    DBCO-PEG3-NHS is a PROTAC linker featuring an alkynyl (DBCO) and N-hydroxysuccinimide (NHS) ester group, facilitating the chemical modification of proteins and antibodies. This reagent is instrumental in the synthesis of PROTACs, enhancing targeted protein degradation applications, as well as contributing to drug delivery systems and the development of biosensors and diagnostic assays. It allows for precise conjugation chemistry, enabling innovative research in therapeutic development and biomolecular interactions.
  44. PROTAC Linkers

    Biotin-PEG8-amine is a biotinylated linker with a polyethylene glycol (PEG) moiety designed for use in PROTAC (Proteolysis Targeting Chimeras) synthesis. This compound enhances the solubility and stability of PROTAC molecules, facilitating targeted protein degradation in cellular studies. Its biotin functionality also allows for efficient capture and purification of PROTACs via streptavidin-based methods, enabling exploration of protein interactions and functional assays in chemical biology.
  45. PROTAC Linker

    Azido-PEG10-NHS ester is a PEG-based linker designed for the synthesis of PROTACs, facilitating targeted protein degradation. This compound features an azide group that enables it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAC) with alkyne-containing molecules. Additionally, it can engage in strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with DBCO or BCN functionalized compounds, making it a versatile tool for chemical biology applications.
  46. PROTAC Linker

    Tert-Butyl 8-hydroxyoctanoate functions as a PROTAC linker, facilitating the synthesis of various PROTACs, including PROTAC CDK Degrader-1. This compound exhibits potent anti-tumor activity through targeted degradation of cyclin-dependent kinases (CDKs), making it a valuable tool for cancer research and therapeutic development. Its role in PROTAC design enhances the specificity and efficacy of targeted protein degradation strategies.
  47. PROTAC Linker

    Biotin-PEG4-methyltetrazine is a PEG-based PROTAC linker designed for the synthesis of targeted protein degradation molecular constructs. This compound features a tetrazine moiety that facilitates click chemistry via an inverse electron demand Diels-Alder reaction (iEDDA) with trans-cyclooctene (TCO) derivatives. Its biological activity allows for the selective recruitment of E3 ligases, making it a valuable tool for researchers studying protein regulation and degradation pathways. This reagent is essential for the development of innovative therapies utilizing PROTAC technology.
  48. PROTAC Linker

    Bromo-PEG3-C2-acid is a polyethylene glycol (PEG)-based linker designed for PROTAC (Proteolysis Targeting Chimera) synthesis. This compound facilitates the formation of PROTACs by providing a suitable structure for the recruitment of E3 ligases and target proteins, enabling targeted degradation in cellular systems. It is suitable for use in research applications focused on protein degradation and modulation of cellular pathways.
  49. PROTAC Linker

    Aminooxy-PEG1-propargyl is a PEG-based linker designed for use in PROTAC (proteolysis-targeting chimera) synthesis. Featuring an alkyne group, it facilitates click chemistry and can participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc), allowing for precise conjugation with azide-containing molecules. This compound is valuable for researchers engaged in the development of targeted protein degradation strategies. Its versatility makes it an essential tool for advancing chemical biology applications.
  50. PROTAC Linker

    HS-PEG5-CH2CH2NH2 hydrochloride is a PROTAC linker designed to facilitate the degradation of target proteins via the proteasome pathway. As part of the polyethylene glycol (PEG) class, this compound provides favorable solubility and biocompatibility, making it an ideal choice for synthesizing PROTAC molecules. Its application supports studies in targeted protein degradation and therapeutic development in various diseases.

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