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His-Trp activation switch

" in MedChemExpress (MCE) Product Catalog:
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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-33821
    LXRβ ligand 1

    		LXR Others
    LXRβ ligand 1 is a LXR β ligand-binding domain agonist, with an EC50 of 57 μM and a Ki of 28 μM against human LXR β. LXRβ ligand 1 forms hydrogen bonds with His435, stabilizes the His-Trp activation switch, and locks the ligand-binding domain in an agonist conformation; its tert-butyl moiety occupies a hydrophobic subpocket, while its phenyl moiety forms a π-π stacking interaction with Phe329. LXRβ ligand 1 serves as a structural unit for the development of LXRβ modulators .
    LXRβ ligand 1

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