GSK3987 |
| Katalog-Nr.GC48610 |
GSK3987 ist ein Pan-LXRα/β-Agonist mit EC50s von 50 nM, 40 nM fÜr LXRα-SRC1 bzw. LXRβ-SRC1.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 264206-85-1
Sample solution is provided at 25 µL, 10mM.
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GSK3987 is a dual agonist of liver X receptor α (LXRα) and LXRβ.1 It recruits steroid receptor coactivator 1 (SRC-1) to LXRα and LXRβ in a ligand-sensing assay (LiSA; EC50s = 50 and 40 nM, respectively). GSK3987 is 50-fold selective for LXRα and LXRβ over a panel of nuclear receptors and GSK3β (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.
1.Jaye, M.C., Krawiec, J.A., Campobasso, N., et al.Discovery of substituted maleimides as liver X receptor agonists and determination of a ligand-bound crystal structureJ. Med. Chem.48(17)5419-5422(2005)
Average Rating: 5 (Based on Reviews and 18 reference(s) in Google Scholar.)
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