E3 Ligase Ligands

E3 ligase ligands bind ubiquitin ligases such as cereblon and von Hippel-Lindau (VHL) in degrader design. In a degrader, they anchor the ligase end of the molecule. E3 ubiquitin ligases transfer ubiquitin to substrate proteins and mark them for degradation by the proteasome. Thalidomide and its analogs bind cereblon (CRBN), a substrate receptor of a cullin-based E3 ligase complex identified as their direct target in 2010. The category includes cereblon ligands such as thalidomide fluoride and TD-106, and VHL ligands such as VL285 and VH032-cyclopropane-F. These ligands are used to build proteolysis-targeting chimeras (PROTACs) and to study how ligases are recruited to new substrates.

Items 101-125 of 922

  • VH032-C4-NH-Boc
    Cat. No.
    A80246

    VH032-C4-NH-Boc

    VH032-C4-NH-Boc is a Boc-modified variant of the VH032 compound that serves as a ligand for the von Hippel-Lindau (VHL) protein, facilitating the recruitment of VHL in E3 ligase applications. Upon exposure to acidic conditions, the Boc protecting group is removed, enabling its use in the synthesis of PROTAC molecules. This compound is a critical intermediate for developing PROTAC strategies that leverage VHL ligands for targeted protein degradation research.

    Out of stock

    All 3 sizes
  • VH032-PEG2-NH-BOC
    Cat. No.
    A80265

    VH032-PEG2-NH-BOC

    VH032-PEG2-NH-BOC is a Boc-modified VH032 compound that functions as a ligand for E3 ligase von Hippel-Lindau (VHL). This reagent facilitates the recruitment of VHL proteins and can be deprotected under acidic conditions, enabling its direct application in PROTAC molecule synthesis. VH032-PEG2-NH-BOC serves as a crucial intermediate for generating PROTACs utilizing VHL ligands, thereby advancing research in targeted protein degradation and therapeutic applications.

    Out of stock

    All 3 sizes
  • CRBN Ligand-Linker Conjugate 2
    Cat. No.
    A80272

    CRBN Ligand-Linker Conjugate 2

    CRBN Ligand-Linker Conjugate 2 is an E3 ligand-linker conjugate designed for the synthesis of proteolysis-targeting chimeras (PROTACs). This compound facilitates targeted degradation of specific proteins by harnessing the ubiquitin-proteasome system. It has been utilized in the development of FIP22, a highly selective IRAK4 PROTAC degrader, which demonstrates potential therapeutic activity against atopic dermatitis. Researchers can leverage this conjugate for advancements in targeted protein degradation strategies.

    Out of stock

    All 3 sizes
  • VH032-O-C2-NH-Boc
    Cat. No.
    A80291

    VH032-O-C2-NH-Boc

    VH032-O-C2-NH-Boc is a Boc-modified derivative of VH032, functioning as a ligand for the E3 ubiquitin ligase von Hippel-Lindau (VHL). This compound facilitates the recruitment of VHL proteins and is valuable in the synthesis of PROTAC (Proteolysis Targeting Chimera) molecules. The Boc protective group can be removed under acidic conditions, allowing for efficient integration into PROTAC development and research applications focused on targeted protein degradation.

    Out of stock

    All 3 sizes
  • Lenalidomide 4'-PEG1-azide
    Cat. No.
    A80293

    Lenalidomide 4'-PEG1-azide

    Lenalidomide 4'-PEG1-azide is a lenalidomide-derived azide designed for use in click chemistry applications. This compound features an azide moiety that engages in copper-catalyzed azide-alkyne cycloaddition (CuAAc) with alkyne-containing molecules, facilitating efficient bioconjugation. Additionally, it can participate in strain-promoted alkyne-azide cycloaddition (SPAAC) with DBCO or BCN-containing partners, making it valuable for various chemical biology studies and the development of novel therapeutics.

    Out of stock

    All 3 sizes
  • Lenalidomide 4'-PEG2-azide
    Cat. No.
    A80301

    Lenalidomide 4'-PEG2-azide

    Lenalidomide 4'-PEG2-azide is a Lenalidomide-derived ligand that targets Cereblon, facilitating the recruitment of CRBN protein. This compound can be utilized to create PROTACs by linking it to various proteins, thereby enabling targeted protein degradation and advancing research in drug development and cellular regulation. Its use is relevant in the study of E3 ligase-mediated pathways and therapeutic strategies in oncology and immunology.

    10 mg
    $280.00
    25 mg
    $540.00
    All 2 sizes
  • VH 101 phenol-alkylC6-amine dihydrochloride
    Cat. No.
    A80375

    VH 101 phenol-alkylC6-amine dihydrochloride

    VH 101 phenol-alkylC6-amine dihydrochloride is a functionalized ligand targeting the von-Hippel-Lindau (VHL) protein, facilitating the development of PROTACs. This compound promotes selective protein degradation by engaging E3 ligases, making it a valuable tool for studying protein turnover and cellular regulation. Its application in chemical biology can aid in understanding the mechanisms of targeted protein degradation and potential therapeutic interventions.

    25 mg
    $485.00
    50 mg
    $820.00
    All 4 sizes
  • Pomalidomide 4'-PEG5-azide
    Cat. No.
    A80415

    Pomalidomide 4'-PEG5-azide

    Pomalidomide 4'-PEG5-azide is a Pomalidomide-derived ligand specifically targeting the cereblon (CRBN) protein. This compound facilitates the recruitment of CRBN, making it a valuable tool in the development of PROTACs by linking to proteins through a suitable linker. Its application in chemical biology research enhances understanding of protein degradation pathways and E3 ligase modulation.

    25 mg
    $360.00
    All 1 sizes
  • E3 ligase Ligand 79
    Cat. No.
    A80443

    E3 ligase Ligand 79

    E3 ligase Ligand 79 serves as a ligand for the CRBN E3 ligase, facilitating the development of targeted protein degradation strategies. This compound is crucial for the synthesis of PROTAC CDK2/4 Degrader-1, which allows for selective degradation of protein targets in various biological contexts. Researchers can utilize this ligand to study the mechanisms of E3 ligase-mediated degradation and its potential therapeutic applications.

    50 mg
    $240.00
    100 mg
    $375.00
    All 5 sizes
  • PT-179
    Cat. No.
    A80444

    PT-179

    PT-179 is a selective cereblon ligand that facilitates targeted protein degradation without off-target effects commonly associated with Thalidomide derivatives. It binds specifically to cereblon, forming a ternary complex with proteins fused to zinc finger degrons, thereby promoting their degradation. This compound demonstrates efficient degradation of proteins tagged with SD40 or SD36, achieving DC50 values of 4.5 nM and 14.3 nM for eGFP, respectively. PT-179 is valuable for developing advanced protein degradation systems in cellular and molecular biology research.

    1 mg
    $40.00
    5 mg
    $100.00
    All 8 sizes
  • VH032
    Cat. No.
    A80445

    VH032

    VH032 is a potent ligand for the von Hippel-Lindau (VHL) protein, acting primarily by inhibiting the interaction between VHL and hypoxia-inducible factor 1-alpha (HIF-1α). Its high affinity and specificity make VH032 an essential tool for research applications involving targeted protein degradation through PROTAC technology. This compound facilitates the study of VHL-mediated pathways and the regulation of hypoxic responses in various biological contexts.

    1 mg
    $30.00
    2 mg
    $45.00
    All 7 sizes
  • Golcadomide
    Cat. No.
    A80446

    Golcadomide

    Synonyms: CC-99282

    Golcadomide is a potent modulator of the CRBN E3 ligase, functioning as a CELMoD that promotes the ubiquitin-mediated proteasomal degradation of key transcription factors such as Ikaros and Aiolos through its interaction with the CRL4 CRBN substrate receptor. This compound has significant biological activity in cancer research, particularly in the study of chronic lymphocytic leukemia (CLL) and non-Hodgkin lymphoma (NHL). Golcadomide's unique mechanism positions it as a valuable tool for exploring therapeutic pathways in hematological malignancies.

    1 mg
    $130.00
    5 mg
    $340.00
    All 6 sizes
  • Lenalidomide-5-aminomethyl hydrochloride
    Cat. No.
    A80447

    Lenalidomide-5-aminomethyl hydrochloride

    Lenalidomide-5-aminomethyl hydrochloride is a derivative of Lenalidomide that acts as a ligand for the E3 ubiquitin ligase cereblon (CRBN). This compound facilitates the recruitment of CRBN to target proteins, enabling targeted protein degradation through the formation of PROTACs (proteolysis-targeting chimeras). It is a valuable tool for researchers exploring protein homeostasis and therapeutic applications in cancer and other diseases where modulation of protein levels is critical.

    100 mg
    $30.00
    250 mg
    $45.00
    All 5 sizes
  • E3 ligase Ligand 32
    Cat. No.
    A80448

    E3 ligase Ligand 32

    E3 Ligase Ligand 32 is a selective ligand for E3 ubiquitin ligase, facilitating the targeted degradation of specific proteins via the PROTAC approach. This compound can be conjugated with a protein ligand through a linker to create innovative PROTACs, such as the SMARCA2/4-degrader-29. E3 Ligase Ligand 32 is valuable for research into protein regulation and degradation pathways, enabling studies in cancer biology and therapeutic development.

    100 mg
    $45.00
    250 mg
    $60.00
    All 6 sizes
  • E3 ligase Ligand 63
    Cat. No.
    A80449

    E3 ligase Ligand 63

    E3 Ligase Ligand 63 is an E3 ligase ligand that facilitates the synthesis of targeted protein degraders, including CDK2 degrader 2. This compound is instrumental in research applications focused on targeted protein degradation and ubiquitin-proteasome system modulation. Its use enables scientists to explore novel therapeutic strategies by selectively regulating protein levels in various biological contexts.

    100 mg
    $30.00
    250 mg
    $50.00
    All 6 sizes
  • CRBN ligand-547
    Cat. No.
    A80450

    CRBN ligand-547

    CRBN ligand-547 is a ligand for the E3 ubiquitin ligase cereblon (CRBN), facilitating the recruitment of the CRBN protein. This compound can be conjugated to a target protein ligand through a linker, enabling the development of Proteolysis Targeting Chimeras (PROTACs). Its specific mechanism of action supports research in targeted protein degradation and the modulation of cellular pathways.

    100 mg
    $25.00
    250 mg
    $40.00
    All 7 sizes
  • ALV2
    Cat. No.
    A80451

    ALV2

    ALV2 is a potent and selective Helios degrader that functions as a molecular glue. It exhibits an IC50 of 0.57 μM for binding to cereblon (CRBN). By targeting Helios, a zinc-finger transcription factor, ALV2 plays a crucial role in regulating the stability of Treg cell phenotype within the inflammatory tumor microenvironment, making it valuable for research in immunology and cancer therapy.

    5 mg
    $370.00
    10 mg
    $670.00
    All 5 sizes
  • 5-Norbornene-2-methylamine
    Cat. No.
    A80452

    5-Norbornene-2-methylamine

    Synonyms: JBP

    5-Norbornene-2-methylamine is a hydrophobic tag utilized in the synthesis of targeted protein degraders. As an E3 ligase ligand, it facilitates the construction of PROTAC molecules, including PROTAC PARP1 degrader-4. This compound is essential for advancing research in protein degradation and its applications in therapeutic development.

    1 g
    $25.00
    5 g
    $60.00
    All 6 sizes
  • CRBN ligand-880
    Cat. No.
    A80453

    CRBN ligand-880

    CRBN ligand-880 is a selective ligand for the E3 ubiquitin ligase cereblon (CRBN), facilitating the recruitment of CRBN to target proteins. This compound can be utilized in the design of PROTACs (proteolysis-targeting chimeras) by linking it to a ligand that binds a specific target protein, enabling targeted protein degradation. Its application in chemical biology research includes elucidating protein function and modulating cellular pathways through controlled degradation mechanisms.

    100 mg
    $20.00
    250 mg
    $35.00
    All 8 sizes
  • CRBN ligand-109
    Cat. No.
    A80454

    CRBN ligand-109

    CRBN ligand-109 is a selective ligand for the CRBN E3 ubiquitin ligase, facilitating the development of proteolysis-targeting chimeras (PROTACs). This compound can effectively promote the ubiquitination and subsequent degradation of target proteins, making it a valuable tool in the study of protein regulation and degradation pathways. Its application is critical in drug discovery, particularly in targeting disease-associated proteins for therapeutic intervention.

    25 mg
    $20.00
    50 mg
    $35.00
    All 7 sizes
  • CC-3060
    Cat. No.
    A80455

    CC-3060

    CC-3060 is a Cereblon modulator that facilitates the degradation of ZBTB16, showing a DC50 value of 0.47 nM in HT-1080 cells. This compound engages specific structural degrons across various zinc finger domains, effectively promoting ZBTB16's proteasomal degradation. CC-3060 has potential applications in the study of cellular processes regulated by ZBTB16 and in the development of innovative therapeutic strategies targeting this pathway.

    1 mg
    $100.00
    5 mg
    $255.00
    All 3 sizes
  • Lenalidomide-Br
    Cat. No.
    A80457

    Lenalidomide-Br

    Lenalidomide-Br is an analog of the cereblon (CRBN) ligand Lenalidomide, functioning as a ligand for the E3 ubiquitin ligase. This compound effectively recruits the CRBN protein, facilitating targeted protein degradation. Lenalidomide-Br can be utilized to create PROTACs, such as the PROTAC STAT3 degrader SD-36, expanding its application in studies focused on targeted therapy and protein modulation in various biological contexts.

    100 mg
    $20.00
    250 mg
    $25.00
    All 3 sizes
  • CCW16
    Cat. No.
    A80458

    CCW16

    CCW16 is a ligand for RNF4, facilitating the synthesis of targeted protein degraders. It serves as a crucial cofactor in the development of PROTACs, such as CCW 28-3, by enhancing the ubiquitination process that promotes protein degradation. This reagent is essential for research involving protein homeostasis and therapeutic development using protein degradation strategies.

    5 mg
    $25.00
    10 mg
    $50.00
    All 5 sizes
  • CRBN ligand-881
    Cat. No.
    A80459

    CRBN ligand-881

    CRBN ligand-881 is a selective ligand for the E3 ubiquitin ligase cereblon (CRBN), facilitating the recruitment of the CRBN protein. This compound can be utilized in the construction of PROTACs (proteolysis-targeting chimeras) by linking it to a target protein ligand through a suitable linker. CRBN ligand-881 is essential for studies involving targeted protein degradation, making it a valuable tool in drug discovery and development research.

    100 mg
    $135.00
    250 mg
    $260.00
    All 3 sizes
  • DCAF1 binder 1
    Cat. No.
    A80460

    DCAF1 binder 1

    DCAF1 binder 1 is a selective ligand for the CRL4 DCAF1 E3 ligase complex. This compound plays a crucial role in targeted protein degradation (TPD), making it valuable for research applications focused on modulating protein levels and understanding the mechanisms of E3 ligase activity. DCAF1 binder 1 can facilitate investigations into the therapeutic potential of TPD in various disease contexts.

    1 mg
    $205.00
    5 mg
    $820.00
    All 6 sizes

Items 101-125 of 922

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