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Fatostatin HBr

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Chemical Structure| 298197-04-3 同义名 : 125B11 hydrobromide;Fatostatin hydrobromide;125B11;Fatostatin (hydrobromide);125B11 HBr
CAS号 : 298197-04-3
货号 : A124858
分子式 : C18H19BrN2S
纯度 : 99%+
分子量 : 375.326
MDL号 : MFCD02376000
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 25 mg/mL(66.61 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 The sterol regulatory-element binding protein (SREBPs) are critical for the production and metabolism of lipids and cholesterol, which are essential for cellular homeostasis and cell proliferation. Fatostatin was recently discovered as a specific inhibitor of SREBP cleavage-activating protein (SCAP), which is required for SREBP activation. Fatostatin possesses antitumor properties including the inhibition of cancer cell proliferation, invasion, and migration, and it arrests cancer cells in G2/M phase[3]. Fatostatin hydrobromide (125B11 hydrobromide) impairs the activation of SREBP-1 and SREBP-2. Fatostatin hydrobromide binds to SCAP (SREBP cleavage-activating protein), and inhibits the ER-Golgi translocation of SREBPs. Fatostatin hydrobromide decreases the transcription of lipogenic genes in cells. Fatostatin hydrobromide possesses antitumor properties, and lowers hyperglycemia in ob/ob mice. Fatostatin hydrobromide (0.1-1 μM; 3 days) inhibits the androgen-independent prostate cancer cell proliferation (IC50=0.1μM) in an independent of the known IGF1-signaling pathway. Fatostatin hydrobromide inhibits insulin-induced adipogenesis of 3T3-L1 cells[4]. Fatostatin hydrobromide (30 mg/kg; 150 mL; i.p.; daily for 28 days) reduces adiposity, ameliorates fatty liver by reducing triglyceride (TG) storage, and lowers hyperglycemia in ob/ob mice[5]. Fatostatin could induce ER degradation by K48-linked polyubiquitination, which was the key mechanism contributing to tamoxifen inhibition of PI3K-AKT-mTOR signalling in breast cancer[6].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
CHO-K1 cells Function assay 20 h Inhibition of SREBP2 activation expressed in CHO-K1 cells co-transfected with pSRE-Luc plasmid assessed as inhibition of luciferase expression after 20 hrs by luciferase reporter gene assay, IC50=5.6 μM 21561152
mouse hepatocytes 1 uM Function assay 90 mins Metabolic stability in mouse hepatocytes at 1 uM after 90 mins by LC-MS/MS analysis 21561152
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.66mL

0.53mL

0.27mL

13.32mL

2.66mL

1.33mL

26.64mL

5.33mL

2.66mL
参考文献

[1]Li X, Chen YT, 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]Kamisuki S, Mao Q, et al. A small molecule that blocks fat synthesis by inhibiting the activation of SREBP. Chem Biol. 2009 Aug 28;16(8):882-92.

[3]Ankur A Gholkar,et al. Fatostatin Inhibits Cancer Cell Proliferation by Affecting Mitotic Microtubule Spindle Assembly and Cell Division. J Biol Chem. 2016 Aug 12;291(33):17001-8.

[4]Choi Y, et al. Identification of bioactive molecules by adipogenesis profiling of organic compounds. J Biol Chem. 2003 Feb 28;278(9):7320-4.

[5]Kamisuki S, et al. A small molecule that blocks fat synthesis by inhibiting the activation of SREBP. Chem Biol. 2009 Aug 28;16(8):882-92.

[6]Ying Liu,et al. Fatostatin in Combination with Tamoxifen Induces Synergistic Inhibition in ER-Positive Breast Cancer. Drug Des Devel Ther. 2020 Aug 26;14:3535-3545.