An LXR inverse agonist
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SR9243

Item No. 18420

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[2-(3-bromophenyl)ethyl]-2,4,6-trimethyl-N-[[3’-(methylsulfonyl)[1,1’-biphenyl]-4-yl]methyl]-benzenesulfonamide
CAS Number
1613028-81-1
Molecular Formula
C31H32BrNO4S2
Formula Weight
626.6
Purity
≥95%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMSO: 1 mg/ml
λmax
256 nm
SMILES
CS(C1=CC=CC(C2=CC=C(CN(CCC3=CC=CC(Br)=C3)S(C4=C(C)C=C(C)C=C4C)(=O)=O)C=C2)=C1)(=O)=O
InChi Code
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 Key
FYQFEJFTCLKXTQ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Cayman Chemical
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    Product Description

    The liver X receptors (LXRs) are nuclear receptors that act as ligand-dependent transcription factors.1 They modulate lipid, cholesterol, and carbohydrate metabolism and homeostasis. SR9243 is a cell-permeable LXR inverse agonist that induces LXR-corepressor interaction at nanomolar concentrations.2 It reduces cancer cell viability (IC50 values range from 15 to 104 nM) without cytotoxicity against non-malignant cells.2 SR9243 disrupts the Warburg effect in cancer cells, suppressing the expression of glycolytic and lipogenic genes and reducing glycolytic metabolites and lipid production. It is effective in vivo, blocking glycolytic and lipogenic gene expression and inducing apoptosis in colon cancer xenografts without inducing weight loss in mice.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Gabbi, C., Warner, M., and Gustafsson, J.Ä. Action mechanisms of liver X receptors. Biochem. Biophys. Res. Commun. 446(3), 647-650 (2014).

    2. Flaveny, C.A., Griffett, K., El-Gendy, B.E.D.M., et al. Broad anti-tumor activity of a small molecule that selectively targets the Warburg effect and lipogenesis. Cancer Cell 28(1), 42-56 (2015).