SR-9243

- Overview
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    Background
    
    SR9243 is a liver-X-receptor (LXR) inverse agonist that induces LXR-corepressor interaction. 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. [1]
    LXR (liver X receptor) is a member of the nuclear receptor family of transcription factors. It is an important regulator of glycolysis and lipogenesis enzyme expression.
    In SW620 cells, 1 mM SR9243 treatment for 12 hours induces cell death with a robust increase in caspase 3/7 activation. In addition, SR9243 disrupts the Warburg effect, suppresses lipogenesis gene expression and lipid production in cancer cells without effecting normal cells. [1]
    In colon tumor xenograft, SR9243 substantially and dose-dependently reduces tumor growth, glycolytic (GCK1, PFK2, PFK1 and LDH) and lipogenic (SCD1, FASN, and SREBP1c) enzyme expression without promoting weight loss. SR9243 also blocks tumor growth without causing immune or hepatic toxicity in vivo. [1]
- Properties
  - Categories
    
    inverse agonist of LXR
    
    CAS Number
    
    1613028-81-1
    
    Molecular Formula
    
    C31H32BrNO4S2
    
    Molecular Weight
    
    626.62
    
    Appearance
    
    A solid
    
    Purity
    
    98.00%
    
    Solubility
    
    ≥25.2 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH
    
    Storage
    
    Store at -20°C
    
    SMILES
    
    CC(C=C(C)C=C1C)=C1S(N(CC2=CC=C(C3=CC(C)=CC=C3)C=C2)CCC4=CC=CC(Br)=C4)(=O)=O.O=S=O
    
    * For Research Use Only