Fatostatin

製品コードS9785 バッチS978501

印刷

化学情報

Chemical Structure Synonyms 125B11 Storage
(From the date of receipt)		 3 years -20°C powder
化学式

C18H18N2S
分子量 294.41 CAS No. 125256-00-0
Solubility (25°C)* 体外 DMSO 75 mg/mL (254.74 mM)
Ethanol 75 mg/mL (254.74 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO Corn oil

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 4.000mg/ml (13.59mM) Taking the 1 mL working solution as an example, add 50 μL of 80 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 4.000mg/ml (13.59mM) Taking the 1 mL working solution as an example, add 50 μL of 80 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明

ジアリールチアゾール誘導体であるFatostatin (125B11) は、Sterol regulatory element binding proteins (SREBPs)活性化の特異的阻害剤です。FatostatinはSCAP (SREBP開裂活性化タンパク質) に結合し、SREBPのERゴルジ移行を阻害します。Fatostatinは、がん細胞の増殖を抑制し、アポトーシスを促進します。
in vitro

Fatostatin impairs the activation process of sterol regulatory element binding proteins (SREBPs), thereby decreasing the transcription of lipogenic genes in cells. This compound inhibits the ER-Golgi translocation of SREBPs through binding to their escort protein, the SREBP cleavage-activating protein (SCAP), at a distinct site from the sterol-binding domain.
in vivo

Fatostatin blocks increases in body weight, blood glucose, and hepatic fat accumulation in obese ob/ob mice, even under uncontrolled food intake. This compound may serve as a tool for gaining further insights into the regulation of SREBP.

プロトコル(参考用のみ)

細胞アッセイ 細胞株 CHO-K1 cells
濃度 20 μM
反応時間 20 h
実験の流れ

CHO-K1 cells are plated out onto a 96-well plate in medium A. The cells are transiently cotransfected with pCMV-PLAP-BP2, pCMV-SCAP, and pAc-b-gal, using Lipofectamine reagent. After incubation for 5 hr, the cells are washed with PBS and then incubated in medium B, in the absence or presence of fatostatin (20 μM) or sterols (10 μg/mL cholesterol and 1 μg/mL 25-hydroxycholesterol). After 20 hr of incubation, an aliquot of the medium is assayed for secreted alkaline phosphatase activity. The cells in each well are lysed and used for measurement of b-galactosidase activities. The alkaline phosphatase activity is normalized by the activity of b-galactosidase.
動物実験 動物モデル 4-to-5-week-old homozygous male obese (ob/ob) mice (C57BL/6J)
投薬量 30 mg/kg
投与方法 IP

参考

  • https://pubmed.ncbi.nlm.nih.gov/19716478/
  • https://pubmed.ncbi.nlm.nih.gov/29436682/

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Visualization and quantification of de novo lipogenesis using a FASN-2A-GLuc mouse model [ Annals of Translational Medicine, September 29, 2022, 958]
Targeting Cholesterol Biosynthesis with Statins Synergizes with AKT Inhibitors in Triple-Negative Breast Cancer [ Cancer Research, October 1, 2024, 3250-3266] PubMed: 39024548
Fatostatin in Combination with Tamoxifen Induces Synergistic Inhibition in ER-Positive Breast Cancer [ Drug Design, Development and Therapy, August 26, 2020, 3535-3545] PubMed: 32921987
Deciphering metabolic reprogramming of immune cells within the tumor microenvironment [ J Transl Med, 2025, 23(1):1055] PubMed: 41053742
SESN2 maintains cartilage homeostasis by SREBP1-mediated lipid metabolism during osteoarthritis progression [ iScience, 2025, 28(8):113097] PubMed: 40822351
SREBP-2 promotes cancer progression through the mevalonate-Akt pathway in non-small cell lung cancer [ Scientific Reports, 2025, 23103] PubMed: 40595126
Hypoxia‑induced SREBP1‑mediated lipogenesis and autophagy promote cell survival via fatty acid oxidation in breast cancer cells [ Oncol Lett, 2025, 29(4):175] PubMed: 39975955
The RORɣ/SREBP2 pathway is a master regulator of cholesterol metabolism and serves as potential therapeutic target in t(4;11) leukemia [ Oncogene, 2024, 43(4):281-293] PubMed: 38030791
Tanshinone IIA acts as a regulator of lipogenesis to overcome osimertinib acquired resistance in lung cancer [ Biochem Pharmacol, 2024, 224:116207] PubMed: 38621425
Cholesterol biosynthesis inhibition synergizes with AKT inhibitors in triple-negative breast cancer [ bioRxiv, 2024, 10.1101/2024.01.16.575899] PubMed: none

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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