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 26-28 of 28

  • Thalidomide-5-Cl
    Cat. No.
    A80701

    Thalidomide-5-Cl

    Thalidomide-5-Cl is a thalidomide analog that serves as a useful tool in research targeting protein degradation via the PROTAC (proteolysis-targeting chimera) mechanism. It exhibits biological activity through its interaction with cereblon, leading to the recruitment of E3 ligases and subsequent ubiquitination of target proteins. This compound is valuable for studies aimed at understanding the modulation of cellular processes and the development of innovative therapeutic strategies.

    50 mg
    $20.00
    100 mg
    $25.00
    All 4 sizes
  • Thalidomide-5-(C6-amine)
    Cat. No.
    A80878

    Thalidomide-5-(C6-amine)

    Thalidomide-5-(C6-amine) is a thalidomide analogue functioning as a PROTAC building block, featuring an E3 ligase ligand with a terminal amine group. This amine group facilitates conjugation reactions with NHS ester groups or carboxylic acids in the presence of coupling agents such as EDC or HATU. Thalidomide-5-(C6-amine) is valuable in the development of bifunctional degraders, supporting research in targeted protein degradation and therapeutic interventions.

    Out of stock

    All 3 sizes
  • 5-Hydrazinyl thalidomide hydrochloride
    Cat. No.
    A81247

    5-Hydrazinyl thalidomide hydrochloride

    5-Hydrazinyl thalidomide hydrochloride is a thalidomide analog that incorporates a hydrazine moiety, facilitating the development of PROTACs that target E3 ligases for the ubiquitination of specific proteins. This compound serves as a versatile intermediate, offering potential for further derivatization through reactions with a variety of carbonyl groups. Its application in chemical biology research holds promise for advancing therapeutic strategies targeting protein degradation pathways.

    25 mg
    $40.00
    50 mg
    $60.00
    All 5 sizes

Items 26-28 of 28

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