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 126-150 of 922

  • VH 101, acid
    Cat. No.
    A80461

    VH 101, acid

    VH 101, acid is a functionalized von-Hippel-Lindau (VHL) protein ligand designed for PROTAC (proteolysis-targeting chimera) research and development. This compound features an E3 ligase ligand along with an alkyl linker equipped with a terminal amine, facilitating conjugation to a target protein ligand. VH 101, acid offers key applications in targeted protein degradation studies, providing insights into therapeutic interventions in various diseases.

    5 mg
    $160.00
    10 mg
    $200.00
    All 5 sizes
  • 5,6-Difluoro-desamino lenalidomide
    Cat. No.
    A80462

    5,6-Difluoro-desamino lenalidomide

    5,6-Difluoro-desamino lenalidomide is a ligand for the E3 ubiquitin ligase cereblon (CRBN), facilitating the recruitment of the CRBN protein to target proteins. This compound serves as a critical building block in the design of PROTACs (proteolysis-targeting chimeras) that harness the ubiquitin-proteasome system for targeted protein degradation. Its unique properties make it valuable for investigating protein modulation and therapeutic strategies in various biological contexts.

    100 mg
    $110.00
    250 mg
    $180.00
    All 4 sizes
  • Lenalidomide-5-Br
    Cat. No.
    A80463

    Lenalidomide-5-Br

    Lenalidomide-5-Br is a derivative of Lenalidomide that functions as a ligand for cereblon (CRBN), an E3 ubiquitin ligase. This compound effectively recruits CRBN to target proteins for ubiquitination and degradation, facilitating the development of Proteolysis Targeting Chimeras (PROTACs). Lenalidomide-5-Br is utilized in research focused on targeted protein degradation and therapeutic development for various diseases, including cancers and autoimmune disorders.

    1 g
    $20.00
    5 g
    $60.00
    All 6 sizes
  • 3-(6-Amino-1-oxoisoindolin-2-yl)piperidine-2,6-dione
    Cat. No.
    A80464

    3-(6-Amino-1-oxoisoindolin-2-yl)piperidine-2,6-dione

    3-(6-Amino-1-oxoisoindolin-2-yl)piperidine-2,6-dione is an analog of Lenalidomide that functions by recruiting the cereblon (CRBN) protein. This compound is primarily utilized in PROTAC (Proteolysis Targeting Chimera) research, enabling targeted degradation of specific proteins to elucidate their biological roles and potential therapeutic avenues. Its unique structure and mechanism make it a valuable tool for advancing studies in drug discovery and targeted therapies.

    25 mg
    $30.00
    50 mg
    $45.00
    All 4 sizes
  • Lenalidomide-I
    Cat. No.
    A80465

    Lenalidomide-I

    Lenalidomide-I is a potent ligand for the E3 ubiquitin ligase cereblon (CRBN). It facilitates the recruitment of the CRBN protein, making it a valuable component for the development of PROTACs (Proteolysis Targeting Chimeras). Applications of Lenalidomide-I include the creation of novel PROTACs, such as the PROTAC BET degrader QCA570, which are utilized in targeted protein degradation research.

    100 mg
    $40.00
    250 mg
    $80.00
    All 3 sizes
  • (S,R,S)-AHPC-propargyl
    Cat. No.
    A80466

    (S,R,S)-AHPC-propargyl

    Synonyms: VH032-propargyl; VHL ligand 7

    (S,R,S)-AHPC-propargyl is a VHL ligand that serves as a crucial component in the development of PROTACs through its role in "click reactions." This compound features an alkyne functional group, enabling it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules. Its versatility makes it valuable for drug discovery and chemical biology applications, particularly in the creation of targeted protein degradation strategies.

    2 mg
    $70.00
    5 mg
    $90.00
    All 6 sizes
  • E3 ligase Ligand 64
    Cat. No.
    A80467

    E3 ligase Ligand 64

    E3 Ligase Ligand 64 functions as a ligand for E3 ligase, enabling its application in targeted protein degradation studies. This compound is instrumental in the synthesis of RP03707, facilitating research in ubiquitin-proteasome pathways and related signaling mechanisms. Its use enhances understanding of E3 ligase activity, making it significant for investigations into disease-related protein dysregulation.

    100 mg
    $30.00
    250 mg
    $60.00
    All 7 sizes
  • (S,S,S)-AHPC hydrochloride
    Cat. No.
    A80468

    (S,S,S)-AHPC hydrochloride

    Synonyms: (S,S,S)-VH032-NH2 hydrochloride

    (S,S,S)-AHPC hydrochloride is a von Hippel-Lindau (VHL) amino building block that serves as a negative control for the (S,R,S)-AHPC compound. This compound is instrumental in studies involving VHL-mediated recruitment of the VHL protein, specifically in the context of targeted therapy and molecular interaction research. Its application extends to investigations requiring a controlled comparison against VHL ligands, providing a vital tool for biochemical analysis.

    5 mg
    $20.00
    10 mg
    $30.00
    All 5 sizes
  • (S,R,S)-AHPC-Boc
    Cat. No.
    A80469

    (S,R,S)-AHPC-Boc

    Synonyms: VH032-Boc

    (S,R,S)-AHPC-Boc is a ligand that selectively targets the von Hippel-Lindau (VHL) protein, facilitating the recruitment of this E3 ligase. This compound is integral to the development of Proteolysis Targeting Chimeras (PROTACs), enabling the selective degradation of target proteins in cellular systems. Its utility in research applications includes studying protein homeostasis and exploring therapeutic strategies for various diseases.

    10 mg
    $25.00
    25 mg
    $50.00
    All 6 sizes
  • CRBN ligand-13
    Cat. No.
    A80470

    CRBN ligand-13

    CRBN ligand-13 acts as a ligand for the CRBN-type E3 ubiquitin ligase, facilitating targeted protein degradation via the PROTAC (Proteolysis Targeting Chimeras) approach. It plays a critical role in the development of novel therapeutic strategies for various diseases by enabling the selective elimination of specific proteins within cells. This compound is valuable for researchers focused on protein regulation and targeted drug development.

    25 mg
    $20.00
    50 mg
    $30.00
    All 8 sizes
  • PD 4'-oxyacetic acid
    Cat. No.
    A80471

    PD 4'-oxyacetic acid

    PD 4'-oxyacetic acid is a carboxylic acid-functionalized ligand for cereblon, a critical component in the development of PROTAC (Proteolysis Targeting Chimeras) degraders. This compound facilitates targeted protein degradation, making it valuable for research applications focused on protein homeostasis and therapeutic intervention in cancer and other diseases. Its ability to engage with the cereblon E3 ubiquitin ligase complex enhances the potential for novel therapeutic strategies in drug discovery.

    10 mg
    $40.00
    25 mg
    $70.00
    All 5 sizes
  • Lenalidomide-OH
    Cat. No.
    A80472

    Lenalidomide-OH

    Lenalidomide-OH is a potent analog of the cereblon (CRBN) ligand Lenalidomide, designed to selectively engage E3 ubiquitin ligase. This compound facilitates the recruitment of CRBN protein, essential for targeted protein degradation applications. Lenalidomide-OH can be coupled with various ligands via a linker to construct PROTACs, such as the BTK degrader SJF620, making it a valuable tool in studies of protein homeostasis and therapeutic development.

    50 mg
    $25.00
    100 mg
    $40.00
    All 6 sizes
  • N-Me-Thalidomide 4-fluoride
    Cat. No.
    A80473

    N-Me-Thalidomide 4-fluoride

    N-Me-Thalidomide 4-fluoride is a ligand for E3 ligase, functioning as a tool in targeted protein degradation studies. It plays a critical role in the synthesis of Anti-inflammatory agent 70, which has potential applications in modulating inflammatory pathways. This compound is of significant interest for researchers investigating therapeutic strategies that harness E3 ligase activity in various biological contexts.

    250 mg
    $20.00
    500 mg
    $30.00
    All 3 sizes
  • 5-Aminothalidomide
    Cat. No.
    A80474

    5-Aminothalidomide

    5-Aminothalidomide is an E3 ligase ligand that plays a crucial role in PROTAC technology. This compound facilitates the synthesis of targeted protein degraders, enabling the development of specific PROTACs such as BRD9 Degrader-7. Its ability to modulate protein levels provides valuable insights into proteostasis and therapeutic intervention in various biological studies.

    100 mg
    $20.00
    250 mg
    $25.00
    All 5 sizes
  • 3-(4-Hydroxy-1-oxoisoindolin-2-yl)piperidine-2,6-dione
    Cat. No.
    A80475

    3-(4-Hydroxy-1-oxoisoindolin-2-yl)piperidine-2,6-dione

    3-(4-Hydroxy-1-oxoisoindolin-2-yl)piperidine-2,6-dione is a ligand for the E3 ligase cereblon (CRBN). This compound enables the targeted recruitment of CRBN, facilitating the degradation of specific proteins through the formation of proteolysis-targeting chimeras (PROTACs). It is a valuable tool for studying protein homeostasis and exploring therapeutic strategies in various diseases, including cancer.

    250 mg
    $20.00
    1 g
    $50.00
    All 2 sizes
  • CRBN ligand-397
    Cat. No.
    A80476

    CRBN ligand-397

    CRBN ligand-397 is a ligand for the E3 ubiquitin ligase cereblon (CRBN), facilitating the recruitment of the CRBN protein. This compound can be connected to a target protein ligand through a linker to create a PROTAC, enabling targeted protein degradation. Its utility in research includes the development of innovative therapeutic strategies that exploit the ubiquitin-proteasome system.

    5 mg
    $25.00
    10 mg
    $40.00
    All 5 sizes
  • (S,R,S)-AHPC-Me-NHBoc
    Cat. No.
    A80477

    (S,R,S)-AHPC-Me-NHBoc

    (S,R,S)-AHPC-Me-NHBoc is a selective ligand for the E3 ubiquitin ligase von Hippel-Lindau (VHL), facilitating the recruitment of the VHL protein to target substrates. This compound can be conjugated with target protein ligands through a linker to create an effective PROTAC (Proteolysis Targeting Chimera). Its unique properties make it a valuable tool in the study of targeted protein degradation and related biological pathways.

    50 mg
    $20.00
    100 mg
    $30.00
    All 2 sizes
  • 5-Br-6-F-Desamino lenalidomide
    Cat. No.
    A80478

    5-Br-6-F-Desamino lenalidomide

    5-Br-6-F-Desamino lenalidomide is a ligand for the E3 ubiquitin ligase cereblon (CRBN), facilitating the recruitment of the cereblon protein. This compound can be conjugated with a target protein ligand using a linker, enabling the formation of a PROTAC (proteolysis-targeting chimeras). Its application in targeted protein degradation research offers significant potential for therapeutic intervention in various diseases.

    100 mg
    $70.00
    250 mg
    $115.00
    All 6 sizes
  • DCAF15 ligand-1
    Cat. No.
    A80479

    DCAF15 ligand-1

    DCAF15 ligand-1 is a selective ligand for the E3 ubiquitin ligase DCAF15, facilitating its role in substrate recognition and ubiquitination processes. This compound is pivotal in biochemical studies aimed at understanding the mechanistic pathways involving DCAF15-mediated protein degradation. Additionally, DCAF15 ligand-1 can be utilized in the synthesis of associated compounds, such as IBG1, enhancing its relevance in research applications focused on targeted protein modulation.

    25 mg
    $455.00
    50 mg
    $720.00
    All 3 sizes
  • KB02-COOH
    Cat. No.
    A80480

    KB02-COOH

    KB02-COOH is a chemical compound that serves as a ligand for E3 ligase, playing a crucial role in the ubiquitin-proteasome system. This fragment is essential for the synthesis of proteolysis-targeting chimeras (PROTACs), including variants such as KB02-JQ1 and KB02-SLF. Researchers can utilize KB02-COOH in studies focused on targeted protein degradation and the modulation of protein activity within cellular pathways.

    5 mg
    $55.00
    10 mg
    $95.00
    All 5 sizes
  • Desamino lenalidomide-6-COOH
    Cat. No.
    A80481

    Desamino lenalidomide-6-COOH

    Desamino lenalidomide-6-COOH is an E3 ubiquitin ligase cereblon (CRBN) ligand that facilitates the recruitment of the cereblon protein. This compound can be conjugated with a target protein ligand through a linker, enabling the development of a PROTAC (Proteolysis Targeting Chimeras). Desamino lenalidomide-6-COOH is essential for research in targeted protein degradation and has potential applications in drug discovery and therapeutic interventions.

    50 mg
    $45.00
    100 mg
    $65.00
    All 6 sizes
  • Desamino lenalidomide-CH2NH2 hydrochloride
    Cat. No.
    A80482

    Desamino lenalidomide-CH2NH2 hydrochloride

    Desamino lenalidomide-CH2NH2 hydrochloride functions as a ligand for the E3 ubiquitin ligase protein cereblon (CRBN). This compound is instrumental in the targeted recruitment of cereblon, facilitating the development of protein-targeted degradation strategies. It can be conjugated with a target protein ligand through a suitable linker to create a proteolysis-targeting chimera (PROTAC), thereby advancing research in protein degradation and targeted therapies.

    100 mg
    $145.00
    250 mg
    $235.00
    All 4 sizes
  • CRBN ligand-734
    Cat. No.
    A80483

    CRBN ligand-734

    CRBN ligand-734 is a potent ligand for the E3 ubiquitin ligase, cereblon (CRBN). This compound facilitates the recruitment of CRBN, enabling targeted protein degradation through the formation of PROTAC (proteolysis-targeting chimeras) by linking it with a target protein ligand via a suitable linker. Its utility is significant in studies focusing on targeted therapy and protein regulation mechanisms in various biological contexts.

    100 mg
    $110.00
    250 mg
    $255.00
    All 4 sizes
  • E3 ligase Ligand PG
    Cat. No.
    A80484

    E3 ligase Ligand PG

    E3 ligase Ligand PG is a selective ligand targeting the CRBN E3 ubiquitin ligase, exhibiting strong binding affinity with an IC50 of 2.191 μM. This compound is suitable for applications involving the recruitment of the CRBN protein, facilitating the development of proteolysis-targeting chimeras (PROTACs). E3 ligase Ligand PG can be utilized in conjunction with BMS-202 to form PROTAC PD-L1 degrader-1, enabling targeted degradation of specific proteins for therapeutic research purposes.

    50 mg
    $25.00
    100 mg
    $40.00
    All 4 sizes
  • (S,R,S)-AHPC-Me dihydrochloride
    Cat. No.
    A80485

    (S,R,S)-AHPC-Me dihydrochloride

    Synonyms: VHL ligand 2 dihydrochloride; E3 ligase Ligand 1 dihydrochloride

    (S,R,S)-AHPC-Me dihydrochloride targets the von Hippel-Lindau (VHL) protein as a ligand for E3 ligase recruitment. This compound serves as a critical precursor for the synthesis of ARV-771, a PROTAC degrader that utilizes the VHL E3 ligase to facilitate the degradation of BET proteins. It has demonstrated potent activity in degrading BET proteins in castration-resistant prostate cancer (CRPC) cells, with a DC50 of less than 1 nM, highlighting its potential for therapeutic applications in cancer research.

    50 mg
    $40.00
    100 mg
    $65.00
    All 5 sizes

Items 126-150 of 922

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