Biochem/physiol Actions

GSK2033 has the ability to repress gluconeogenic gene expression stimulated by GC (glucocorticoids), without altering immune-responsive GR (GC receptor) target genes. It helps to target several nuclear receptors that can alter hepatic gene expression.

GSK2033 is an antagonist of the nuclear receptor liver-X-receptor (LXR) with pIC50 values of 7.0 for LXRα and 7.4 for LXRβ. Treatment of murine CD41 T cells with GSK2033 enhanced cellular proliferation and Th1/Th2/Th17 differentiation. In another study, the conjugated linoleic acid (CLA)-induced expression of efflux protein ATP-binding-cassette transporter A1 (ABCA1) was completely abolished by preincubation with GSK2033, showing that CLA mediated regulation of ABCA-1 expression is LXR dependent.

Packaging

5, 25 mg in glass bottle