"目录号: HY-14452
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Fatostatin是一个SREBP的抑制剂，能够结合SCAP，阻止它的ER-to-Golgi运输，在哺乳动物中IC50分别是2.5 到10 uM之间。
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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.