同义名 :	125B11
	CAS号 :	125256-00-0
	货号 :	A468679
	分子式 :	C18H18N2S
	纯度 :	99%+
	分子量 :	294.41
	MDL号 :	MFCD02376000
	存储条件：	Pure form Inert atmosphere, 2-8°C In solvent -20°C:3-6个月-80°C:12个月
	溶解度 :	-
	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