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Ligand for Target Protein for PROTAC

Ligands for target proteins in PROTAC design bind the protein that a degrader is meant to remove. A proteolysis-targeting chimera (PROTAC) joins such a ligand to an E3 ubiquitin ligase ligand through a linker, so that the ligase ubiquitinates the bound target. Most entries are known inhibitors or receptor ligands modified with an attachment point, such as an aldehyde, amine, carboxylic acid or alkyne group. Dasatinib carbaldehyde and Imatinib carbaldehyde are aldehyde-bearing analogs of two kinase inhibitors. BI-4464 binds protein tyrosine kinase 2 (PTK2), also called focal adhesion kinase (FAK), and SirReal1-O-propargyl carries a propargyl handle on a sirtuin 2 (SIRT2) ligand. Receptor ligands in the list include Estrone-N-O-C1-amido and AP1867-2-(carboxymethoxy), which binds FK506-binding proteins.

1 Item

  • PROTAC ERRα ligand 1
    Cat. No.
    A81279
    CAS No.
    1264754-13-3

    PROTAC ERRα ligand 1

    PROTAC ERRα ligand 1 is an orally active inverse agonist targeting ERRα with an IC50 of 0.6 μM. This compound demonstrates selective inhibition, as it exhibits minimal activity against a range of other nuclear receptors, including ERαc, ERRγ, ERβ, PPARα, PPARγ, PPARδ, and RXRα. PROTAC ERRα ligand 1 is valuable for research in metabolic diseases, such as type 2 diabetes and obesity, and has shown potential in enhancing insulin sensitivity in vivo.

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    1 mg
    $25.00
    2 mg
    $30.00
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