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SR9243

CAS No. : 1613028-81-1

MCE 站：SR9243

产品活性：SR9243 是 liver-X-receptor (LXR) 的反向激动剂，能够诱导 LXR-辅阻遏物相互作用。

研究领域：Metabolic Enzyme/Protease

作用靶点：LXR

In Vitro: SR9243 specifically targets LXR and downregulates LXR-mediated gene expression, dose-dependently suppresses LXRα- and LXRβ-dependent transcription at nanomolar concentrations, and potently inhibits LXR-driven luciferase activity in cultured cancer cells. SR9243 potently reduces cancer cell viability at nanomolar concentrations (IC₅₀ appr 15-104 nM) in prostate (PC3 and!DU-145), colorectal (SW620 and HT29), and lung (HOP-62 and NCI-H23) cancer cell lines. And the colony-forming capacity of cancer cells is also significantly loared by SR9243 in a dose-dependent manner. SR9243 is a potent inhibitor of lipogenic gene expression that selectively kills cancer cells by depleting intracellular lipids. Combination of cancer cell media with oleate, stearate, and palmitate in combination completely rescues cancer cell viability in cancer cells. Fatty acid supplementation also rescues the viability of SW620 cells in which glycolysis is substantially disrupted.

In Vivo: SR9243 is able to profoundly inhibit tumor glycolysis, lipogenesis, and induce apoptotic cancer cell death without promoting weight loss in vivo. SR9243 inhibits tumor growth without profoundly repressing glycolytic gene expression, and inhibits tumor growth and lipogenesis without hepatotoxicity or inflammation in vivo.

相关产品：Bioactive Compound Library Plus  |  Metabolism/Protease Compound Library  |  Anti-Cancer Compound Library  |  Glycolysis Compound Library  |  T0901317  |  GSK2033  |  LXR-623  |  27-Hydroxycholesterol  |  (20S)-Protopanaxatriol  |  SR9238  |  24-Hydroxycholesterol  |  AZ876  |  Saikosaponin A  |  Yamogenin  |  DMHCA  |  Nagilactone B  |  Gymnestrogenin  |  Iristectorigenin B  |  LXRβ agonist-2

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