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.

9 Items

  • Thalidomide-iodo
    Cat. No.
    A80558

    Thalidomide-iodo

    Thalidomide-iodo is an iodo-substituted E3 ligase activator. It plays a crucial role in the ubiquitin-proteasome pathway, facilitating targeted protein degradation. Thalidomide-iodo can serve as a valuable intermediate for further chemical modifications, allowing researchers to explore novel derivatives in the study of protein regulation and cellular processes. This compound is essential for investigations into therapeutic strategies related to various diseases, including cancer and immune disorders.

    100 mg
    $65.00
    250 mg
    $115.00
    All 4 sizes
  • Thalidomide 4-chloro
    Cat. No.
    A80563

    Thalidomide 4-chloro

    Thalidomide 4-chloro is an E3 ligase activator that exhibits unique properties due to its chlorinated structure. This compound plays a significant role in promoting protein degradation pathways, making it valuable for research focused on modulating cellular processes. Additionally, Thalidomide 4-chloro serves as a versatile starting material for further derivatization through chlorine substitution, allowing for the exploration of novel analogs in chemical research.

    500 mg
    $20.00
    1 g
    $30.00
    All 3 sizes
  • Thalidomide-1-Me,5-F
    Cat. No.
    A80582

    Thalidomide-1-Me,5-F

    Thalidomide-1-Me,5-F is a fluorinated E3 ligase activator that functions by promoting the ubiquitination of target proteins. This compound exhibits key biological activity in modulating protein degradation pathways, making it valuable for research in cellular signaling and therapeutic interventions. Additionally, Thalidomide-1-Me,5-F can serve as a substrate for further derivatization via nucleophilic aromatic substitution (SNAr) reactions.

    100 mg
    $25.00
    250 mg
    $50.00
    All 5 sizes
  • Thalidomide-5-Br,6-F
    Cat. No.
    A80744

    Thalidomide-5-Br,6-F

    Thalidomide-5-Br,6-F is a Thalidomide analogue functioning as an E3 ligase activator, promoting the ubiquitination of target proteins for proteolytic degradation. This compound enhances cellular pathways by modulating protein turnover, making it valuable in studies related to protein homeostasis and targeted degradation. Its unique structural features allow for potential further derivatization through substitution at the fluorine or bromine positions, offering avenues for the development of novel reagents.

    25 mg
    $245.00
    50 mg
    $355.00
    All 4 sizes
  • 5-Hydroxy-2-(1-methyl-2,6-dioxopiperidin-3-yl)isoindole-1,3-dione
    Cat. No.
    A80963

    5-Hydroxy-2-(1-methyl-2,6-dioxopiperidin-3-yl)isoindole-1,3-dione

    5-Hydroxy-2-(1-methyl-2,6-dioxopiperidin-3-yl)isoindole-1,3-dione is a Thalidomide analog that possesses a hydroxy group allowing for potential derivatization. This compound functions as an E3 ligase activator, facilitating the ubiquitinylation of target proteins. Its biological activity makes it valuable for research in drug development, particularly in studies focused on protein degradation and cellular signaling pathways.

    25 mg
    $35.00
    50 mg
    $55.00
    All 3 sizes
  • 5-Bromomethylthalidomide
    Cat. No.
    A80973

    5-Bromomethylthalidomide

    5-Bromomethylthalidomide is an E3 ligase activator that facilitates protein ubiquitination, thereby influencing protein stability and degradation pathways. This compound serves as a key tool in research focused on targeted protein degradation and cellular regulation mechanisms. Its potential for further derivatization through bromide substitution enhances its utility in chemical biology and therapeutic research.

    100 mg
    $70.00
    250 mg
    $125.00
    All 4 sizes
  • Thalidomide-4-Br,7-F
    Cat. No.
    A81000

    Thalidomide-4-Br,7-F

    Thalidomide-4-Br,7-F is an E3 ligase activator, containing both bromine and fluorine substituents. E3 ligases play a crucial role in the ubiquitin-proteasome system by tagging proteins for degradation, thereby regulating various cellular processes. This compound's halogen functional groups allow for potential further derivatization, making it a valuable tool for research in protein degradation pathways and targeted protein modulation. Its application extends to studies involving cancer biology, protein regulation, and therapeutic development.

    10 mg
    $70.00
    25 mg
    $125.00
    All 4 sizes
  • Thalidomide-pinacolborane
    Cat. No.
    A81079

    Thalidomide-pinacolborane

    Thalidomide-pinacolborane is a Thalidomide analogue that incorporates a boronic pinacol ester (Bpin group) and serves as an activator for E3 ligases. This compound plays a crucial role in ubiquitination, facilitating the targeted degradation of proteins through proteolytic pathways. Its applications in chemical biology include studies on protein regulation and modulation of cellular signaling processes, making it a valuable tool in research focused on proteostasis and therapeutic interventions.

    5 mg
    $50.00
    10 mg
    $85.00
    All 6 sizes
  • 4-Me-Thalidomide
    Cat. No.
    A81132

    4-Me-Thalidomide

    4-Me-Thalidomide is an E3 ligase activator characterized by the presence of a methyl group. This compound enhances the activity of E3 ligases, which are crucial for tagging proteins with ubiquitin for targeted proteolytic degradation. 4-Me-Thalidomide can be utilized in research applications investigating protein turnover and the ubiquitin-proteasome system, offering insights into cellular processes and disease mechanisms.

    Out of stock

    All 3 sizes

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