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脂肪抑制素 /Fatostatin {[allProObj[0].p_purity_real_show]}

货号:A468679 同义名: 125B11

Fatostatin (125B11) 是一种特异性抑制SREBP激活的抑制剂,阻止SREBP-1和SREBP-2的激活。它与SCAP(SREBP裂解激活蛋白)结合,抑制SREBPs的ER-高尔基体转运,减少细胞中脂质生成基因的转录。Fatostatin具有抗肿瘤特性,并降低ob/ob小鼠的高血糖。

Fatostatin 化学结构 CAS号:125256-00-0
Fatostatin 化学结构
CAS号:125256-00-0
Fatostatin 3D分子结构
CAS号:125256-00-0
Fatostatin 化学结构 CAS号:125256-00-0
Fatostatin 3D分子结构 CAS号:125256-00-0
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Fatostatin 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].

Fatostatin 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

Fatostatin 实验方案

计算器
存储液制备 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

Fatostatin 技术信息

CAS号125256-00-0
分子式C18H18N2S
分子量 294.414
别名 125B11
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,2-8°C

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
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