"目錄號: HY-14452

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Fatostatin是一個SREBP的抑制劑，能夠結合SCAP，阻止它的ER-to-Golgi運輸，在哺乳動物中IC50分別是2.5 到10 uM之間。

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SBE-β-CD-MPTP hydrochloride-Cyclosporin A-Etomoxir-Auranofin-GKT137831-Ceruletide-Acetylcysteine-JC-1-BPTES-Brassinolide-FCCP-IPTG-MTT-RSL3 1S,3R--

生物活性

Description

Fatostatin A is a inhibitor of SREBP that directly binds SCAP and blocks its ER-to-Golgi transport with IC50 of 2.5 and 10 μM in mammalian cellstarget: SREBPIC50: 2.5 ~10 μMIn vitro: Fatostatin A suppress cell proliferation and anchorage-independent colony formation in both androgen-responsive LNCaP and androgen-insensitive C4-2B prostate cancer cells. [1] Fatostatin potently inhibited cell growth.[2]In vivo: Fatostatin A cause G2/M cell cycle arrest and induce apoptosis by increasing caspase-3/7 activity and the cleavages of caspase-3 and PARP. [1] μCT analyses show that fatostatin A treatment preserve bone mass and structure in the proximal tibial trabecular bone in the mouse RANKL-induced bone loss model.[3]

References

[1].Li X et al. Fatostatin displays high antitumor activity in prostate cancer by blocking SREBP-regulated metabolic pathways and androgen receptor signaling. Mol Cancer Ther. 2014 Apr;13(4):855-66.

[2].Shao W et al. Fatostatin blocks ER exit of SCAP but inhibits cell growth in a SCAP-independent manner. J Lipid Res. 2016 Aug;57(8):1564-73.

[3].Inoue K et al. Fatostatin, an SREBP inhibitor, prevented RANKL-induced bone loss by suppression of osteoclast differentiation. Biochim Biophys Acta. 2015 Nov;1852(11):2432-41.