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    SR9243
    SR9243

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1854
    CAS #: 1613028-81-1Purity ≥98%

    Description: SR9243 is a potent and selective inverse agonist of LXR. It potently reduces cancer cell viability (IC50=15–104 nM) in MTT reduction assays in prostate (PC3 and DU-145), colorectal (SW620 and HT29), and lung (HOP-62 and NCI-H23) cancer cell lines. SR9243 kills cancer cells by inhibiting lipid production and the Warburg effect. SR9243 induces cell death in multiple types of cancer and does not cause the side effects that have derailed previous attempts to target these processes.

    References: Cancer Cell. 2015 Jul 13;28(1):42-56.

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    Molecular Weight (MW)626.62 
    FormulaC31H32BrNO4S2 
    CAS No.1613028-81-1 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: <1 mg/mL
    Water: <1 mg/mL
    Ethanol: N/A
    Other info

    Chemical Name: N-(3-bromophenethyl)-2,4,6-trimethyl-N-((3'-(methylsulfonyl)-[1,1'-biphenyl]-4-yl)methyl)benzenesulfonamide

    InChi Key: InChI=1S/C31H32BrNO4S2/c1-22-17-23(2)31(24(3)18-22)39(36,37)33(16-15-25-7-5-9-29(32)19-25)21-26-11-13-27(14-12-26)28-8-6-10-30(20-28)38(4,34)35/h5-14,17-20H,15-16,21H2,1-4H3

    InChi Code: FYQFEJFTCLKXTQ-UHFFFAOYSA-N

    SMILES Code: O=S(C1=C(C)C=C(C)C=C1C)(N(CCC2=CC=CC(Br)=C2)CC3=CC=C(C4=CC=CC(S(=O)(C)=O)=C4)C=C3)=O

    Synonyms

    SR9243; SR-9243; SR 9243


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    In Vitro

    In vitro activity: In HEK293 cells expressing LXRs, SR9243 inhibits LXR activation by enhancing LXR-corepressor recruitment. In a variety of cancer cell types, SR9243 reduces cancer cell viability, induces apoptotic cell death, and sensitizes cancer cells to chemotherapeutic treatments. 


    Cell Assay: Cells are cultured in 96 well plates and treated with designated amounts of SR9243 for 96 hr in media containing 1% FBS and antibiotics. Cell-viability is assessed using the Cell-titre 96 kit according to the manufacturer’s guidelines. Cell culture media is supplemented with oleate, stearate and palmitate dissolved in methanol to a concentration of 25 mM. 25 mM stocks are then diluted 10 fold in PBS containing 0.9% BSA. Lipid stocks (100X) are stored at −20° until needed.

    In VivoIn Ob/Ob mice fed a high-fat diet, SR9243 (60 mg/kg, i.p.) inhibits LXR-dependent lipogenic enzyme gene expression and tumor growth. 
    Animal modelMice bearing SW620, DU-145, or LLC tumors 
    Formulation & DosageFormulated in 10% DMSO, 10% Tween-80;  30, 60 mg/kg, once daily; i.p. injection 
    References

    Cancer Cell. 2015 Jul 13;28(1):42-56. 


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    SR9243

    SR9243 Is an LXR Inverse Agonist that Induces Corepressor Recruitment. Cancer Cell. 2015 Jul 13;28(1):42-56.
     

    SR9243

    SR9243 Inhibits Glycolytic Lipogenic Enzymes in Cancer Cells. Cancer Cell. 2015 Jul 13;28(1):42-56.
     

    SR9243

    SR9243 Reduces Tumor Growth, Glycolytic and Lipogenic Enzyme Expression in Tumors In Vivo. Cancer Cell. 2015 Jul 13;28(1):42-56.


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