GSK3987

GSK3987

CAT N°: 30954
Price:

591.00 502.35

GSK3987 is a dual agonist of liver X receptor ? (LXR?) and LXR?.{57442} It recruits steroid receptor coactivator 1 (SRC-1) to LXR? and LXR? in a ligand-sensing assay (LiSA; EC50s = 50 and 40 nM, respectively). GSK3987 is 50-fold selective for LXR? and LXR? over a panel of nuclear receptors and GSK3? (IC50 = >5,000 nM) but does induce ABCA1 expression in a reporter assay using THP-1 cells (EC50 = 80 nM). It inhibits LPS-induced IL-6 secretion in THP-1 macrophages. GSK3987 increases the expression of the sterol regulatory element binding protein 1c (SREBP-1c) and induces triglyceride accumulation in HepG2 cells in a concentration-dependent manner.

Territorial Availability: Available through Bertin Technologies only in France

  • Synonyms
    • 3-[(4-methoxyphenyl)amino]-4-phenyl-1-(phenylmethyl)-1H-pyrrole-2,5-dione
  • Correlated keywords
    • GSK 3987 LXR SRC1 GSK 3? GSK3 ? ABCA THP1 IL6 interleukin SREBP1c Hep G2 HepG 2
  • Product Overview:
    GSK3987 is a dual agonist of liver X receptor ? (LXR?) and LXR?.{57442} It recruits steroid receptor coactivator 1 (SRC-1) to LXR? and LXR? in a ligand-sensing assay (LiSA; EC50s = 50 and 40 nM, respectively). GSK3987 is 50-fold selective for LXR? and LXR? over a panel of nuclear receptors and GSK3? (IC50 = >5,000 nM) but does induce ABCA1 expression in a reporter assay using THP-1 cells (EC50 = 80 nM). It inhibits LPS-induced IL-6 secretion in THP-1 macrophages. GSK3987 increases the expression of the sterol regulatory element binding protein 1c (SREBP-1c) and induces triglyceride accumulation in HepG2 cells in a concentration-dependent manner.

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