An antagonist of LXRα and LXRβ
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GSK2033

Item No. 25443

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2,4,6-trimethyl-N-[[3'-(methylsulfonyl)[1,1'-biphenyl]-4-yl]methyl]-N-[[5-(trifluoromethyl)-2-furanyl]methyl]-benzenesulfonamide
CAS Number
1221277-90-2
Molecular Formula
C29H28F3NO5S2
Formula Weight
591.7
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMF: 5 mg/mlDMSO: 1 mg/mlEthanol: Slightly soluble
λmax
255 nm
SMILES
CC1=CC(C)=C(S(N(CC2=CC=C(C3=CC=CC(S(C)(=O)=O)=C3)C=C2)CC4=CC=C(C(F)(F)F)O4)(=O)=O)C(C)=C1
InChi Code
InChI=1S/C29H28F3NO5S2/c1-19-14-20(2)28(21(3)15-19)40(36,37)33(18-25-12-13-27(38-25)29(30,31)32)17-22-8-10-23(11-9-22)24-6-5-7-26(16-24)39(4,34)35/h5-16H,17-18H2,1-4H3
InChi Key
PSOXOVKYGWBTPB-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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    OBESITY RESEARCH SOLUTIONS
    Product Description

    GSK2033 is an antagonist of liver X receptor α (LXRα) and LXRβ (IC50s = 0.1 and 0.398 µM, respectively) that has no agonist activity in an LXR transactivation assay.1 It inhibits LXR agonist-induced and basal expression of the LXR target genes ATP-binding cassette transporter 1 (ABCA1) and sterol regulatory element binding protein 1c (SREBP-1c) in THP-1 and HepG2 cells, respectively. However, GSK2033 binds promiscuously to a variety of nuclear receptors including RORγ, RXRα, ERα, and ERβ in a nuclear receptor specificity assay in HEK293 cells and, in a mouse model of non-alcoholic fatty liver disease (NAFLD), it induces the expression of fatty acid synthase and SREBP-1.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Zuercher, W.J., Buckholz, R.G., Campobasso, N., et al. Discovery of tertiary sulfonamides as potent liver X receptor antagonists. J. Med. Chem. 53(8), 3412-3416 (2010).

    2. Griffett, K., and Burris, T.P. Promiscuous activity of the LXR antagonist GSK2033 in a mouse model of fatty liver disease. Biochem. Biophys. Res. Commun. 479(3), 424-428 (2016).