Fatostatin HBr

製品コードS8284 バッチS828404

印刷

化学情報

Synonyms

125B11 HBr

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₁₈H₁₈N₂S·HBr

分子量

375.33

CAS No.

298197-04-3

Solubility (25°C)*

体外

DMSO

38 mg/mL (101.24 mM)

Ethanol (warmed with 50ºC water bath)

5 mg/mL (13.32 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 1 40%PEG300 2 5%Tween80 3 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。	1.500mg/ml (4.00mM)	Taking the 1 mL working solution as an example, add 50 μL of 30 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	Fatostatin HBr is an inhibitor of sterol regulatory element binding protein (SREBP). It impairs the activation of SREBP-1 and SREBP-2.
in vitro	Fatostatin inhibits the insulin-induced adipogenesis of 3T3-L1 cells and the serum-independent growth of human androgen-independent prostate cancer (DU145) cells. Fatostatin blocks the activation of SREBPs in cells in tissue culture^[1]. Fatostatin suppresses cell proliferation and anchorage-independent colony formation in both androgen-responsive LNCaP and androgen-insensitive C4-2B prostate cancer cells. Fatostatin also reduced in vitro invasion and migration in both cell lines. Further, fatostatin causes G2/M cell cycle arrest and induces apoptosis by increasing caspase-3/7 activity and the cleavages of caspase-3 and PARP^[2].
in vivo	Fatostatin blocks increases in body weight, blood glucose, and hepatic fat accumulation in obese ob/ob mice, even under uncontrolled food intake^[1]. Fatostatin significantly inhibits subcutaneous C4-2B tumor growth and markedly decreases serum PSA level compared to the control group^[2].

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	On day 0, CHO-K1 cells are plated out onto a 96-well plate in medium A. On day 2, the cells are transiently cotransfected with pCMV-PLAP-BP2(513–1141), pCMV-SCAP, and pAc-β-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 β-galactosidase activities. The alkaline phosphatase activity is normalized by the activity of β-galactosidase.
動物実験	動物モデル	Obese (ob/ob) mice (C57BL/6J background)
	投薬量	30 mg/kg
	投与方法	i.p.

参考

https://pubmed.ncbi.nlm.nih.gov/19716478/
https://pubmed.ncbi.nlm.nih.gov/24493696/

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：

Lipid metabolism reprograming by SREBP1-PCSK9 targeting sensitizes pancreatic cancer to immunochemotherapy [ Cancer Commun (Lond), 2025, 10.1002/cac2.70038]	PubMed: 40439109
Lactate shuttle between cytotrophoblast and syncytiotrophoblast in the placenta enhances ferroptosis resistance and maintains placental homeostasis: implications for early pregnancy loss [ Cell Commun Signal, 2025, 23(1):438]	PubMed: 41088442
The Effect of Rumen-Protected Conjugated Linoleic Acid on Milk Composition and Milk Energy Output of Holstein Cows and Its Potential Mechanism [ ACS Omega, 2024, 9(47):47042-47051]	PubMed: 39619548
NFYC-37 promotes tumor growth by activating the mevalonate pathway in bladder cancer [ Cell Rep, 2023, 42(8):112963]	PubMed: 37561631
TGF-β1 promotes SCD1 expression via the PI3K-Akt-mTOR-SREBP1 signaling pathway in lung fibroblasts [ Respir Res, 2023, 24(1):8]	PubMed: 36627645
Visualization and quantification of de novo lipogenesis using a FASN-2A-GLuc mouse model [ Ann Transl Med, 2022, 10(18):958]	PubMed: 36267736
Targeting immunosuppressive macrophages overcomes PARP inhibitor resistance in BRCA1-associated triple-negative breast cancer [ Nat Cancer, 2021, 2(1):66-82]	PubMed: 33738458
Targeting immunosuppressive macrophages overcomes PARP inhibitor resistance in BRCA1-associated triple-negative breast cancer [ Nat Cancer, 2021, 2(1):66-82]	PubMed: 33738458
Pharmacological inhibition of fatty acid synthesis blocks SARS-CoV-2 replication [ Nat Metab, 2021, 10.1038/s42255-021-00479-4]	PubMed: 34580494
p53 transcriptionally regulates SQLE to repress cholesterol synthesis and tumor growth [ EMBO Rep, 2021, e52537]	PubMed: 34459531

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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