脂肪抑制素 /Fatostatin
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货号：A468679
同义名：
125B11
Fatostat in (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SREBP s的ER-高尔基体转运，减少细胞中脂质生成基因的转录。Fatostat in具有抗肿瘤 特性，并降低ob/ob小鼠的高血糖。
Fatostatin 化学结构
Fatostatin 3D分子结构
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货号：A468679
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Fatostatin 质控信息
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] [4] [5] [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
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Fatostatin 实验方案
计算器
摩尔计算器
总药量计算器
工作液计算器
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
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