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Fatostatin

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Chemical Structure| 125256-00-0 同义名 : 125B11
CAS号 : 125256-00-0
货号 : A468679
分子式 : C18H18N2S
纯度 : 99%+
分子量 : 294.414
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(84.91 mM)，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 Fatostatin is an inhibitor of SREBP that directly binds SCAP (SREBP cleavage-activating protein) and blocks its ER-to-Golgi transport with IC50 of 2.5 and 10 μM in mammalian cells. Fatostatin blocked increases in body weight, blood glucose, and hepatic fat accumulation in obese ob/ob mice, even under uncontrolled food intake[3]. In vitro analysis revealed that fatostatin significantly inhibited the secretion of inflammatory cytokines from cells activated with lipopolysaccharide, without affecting cell viability[4]. Fatostatin inhibited tubulin polymerization, arrested cells in mitosis, activated the spindle assembly checkpoint, and triggered mitotic catastrophe and reduced cell viability[5]. Fatostatin, an inhibitor of SREBP1, could increase the sensitivity of endometrial cancer to progesterone and reverse progesterone resistance by inhibiting SREBP1 both in vitro and in vivo[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.40mL

0.68mL

0.34mL

16.98mL

3.40mL

1.70mL

33.97mL

6.79mL

3.40mL
参考文献

[1]Shao W, Machamer CE, 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.

[2]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.

[3]Kamisuki S, Mao Q, Abu-Elheiga L, Gu Z, Kugimiya A, Kwon Y, Shinohara T, Kawazoe Y, Sato S, Asakura K, Choo HY, Sakai J, Wakil SJ, Uesugi M. A small molecule that blocks fat synthesis by inhibiting the activation of SREBP. Chem Biol. 2009 Aug 28;16(8):882-92

[4]Ma S, Murakami K, Tanaka K, Hashimoto M, Tanaka M, Kitagori K, Akizuki S, Nakashima R, Yoshifuji H, Ohmura K, Morinobu A, Mimori T. Fatostatin ameliorates inflammation without affecting cell viability. FEBS Open Bio. 2022 Mar;12(3):594-604

[5]Gholkar AA, Cheung K, Williams KJ, Lo YC, Hamideh SA, Nnebe C, Khuu C, Bensinger SJ, Torres JZ. Fatostatin Inhibits Cancer Cell Proliferation by Affecting Mitotic Microtubule Spindle Assembly and Cell Division. J Biol Chem. 2016 Aug 12;291(33):17001-8

[6]Ma X, Zhao T, Yan H, Guo K, Liu Z, Wei L, Lu W, Qiu C, Jiang J. Fatostatin reverses progesterone resistance by inhibiting the SREBP1-NF-κB pathway in endometrial carcinoma. Cell Death Dis. 2021 May 26;12(6):544