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GAC0001E5

Chemical Structure : GAC0001E5

CAS No.: 927969-67-3

GAC0001E5 (LXR ligand 1E5)

Catalog No.: PC-49867Not For Human Use, Lab Use Only.

GAC0001E5 (LXR ligand 1E5) is a small molecule liver X receptor (LXR) inverse agonist and a potent inhibitor of pancreatic and breast cancer cells (MDA-MB-231, IC50=7.74 uM).

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    Biological Activity

    GAC0001E5 (LXR ligand 1E5) is a small molecule liver X receptor (LXR) inverse agonist and a potent inhibitor of pancreatic and breast cancer cells (MDA-MB-231, IC50=7.74 uM).
    GAC0001E5 significantly decreased LXRβ transcription and translation in MCF7-TamR and MDA-MB-231 cells.
    GAC0001E5 induces oxidative stress in breast cancer cells, disrupting glutaminolysis, downregulates the intracellular glutamate levels.
    Combination treatment of 1E5 with GLS inhibitor BPTES synergistically decreases glutaminolysis and growth of PDAC cells.

    Physicochemical Properties

    M.Wt 331.30
    Formula C17H12F3N3O
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20°C 12 Months; 4°C 6 Months
    In Solvent
    -80°C 6 Months; -20°C 6 Months
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

    6-phenyl-2-((3-(trifluoromethyl)phenyl)amino)pyrimidin-4(3H)-one

    References

    1. Srivastava S, et al. Int J Mol Sci. 2020 Dec 17;21(24):9622.

    2. Premaratne A, et al. Biomolecules. 2023 Feb 10;13(2):345.

    3. araboga H, et al.ACS Chem. Biol. 2020;15:2916–2928.

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