Fatostatin HBr

Catalog No.S8284 Batch:S828401

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Technical Data

Formula

C18H18N2S·HBr
Molecular Weight 375.33 CAS No. 298197-04-3
Solubility (25°C)* In vitro Ethanol 58 mg/mL (154.53 mM)
DMSO 7 mg/mL (18.65 mM)
Water Insoluble
* <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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description Fatostatin HBr is an inhibitor of sterol regulatory element binding protein (SREBP). It impairs the activation of SREBP-1 and SREBP-2.
Targets
SREBPs [1]
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].

Protocol (from reference)

Cell Assay:[1]
  • Cell lines

    CHO-K1 cells

  • Concentrations

    20 μM

  • Incubation Time

    20 h

  • Method

    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.
Animal Study:[1]
  • Animal Models

    Obese (ob/ob) mice (C57BL/6J background)

  • Dosages

    30 mg/kg

  • Administration

    i.p.

Selleck's Fatostatin HBr has been cited by 13 publications

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
Genetic Screens Identify Host Factors for SARS-CoV-2 and Common Cold Coronaviruses [ Cell, 2020, S0092-8674(20)31626-3] PubMed: 33333024
Fatostatin in Combination with Tamoxifen Induces Synergistic Inhibition in ER-Positive Breast Cancer [ Drug Des Devel Ther, 2020, 14:3535-3545] PubMed: 32921987
Staphylococcal Enterotoxin C2 Mutant-Directed Fatty Acid and Mitochondrial Energy Metabolic Programs Regulate CD8+ T Cell Activation [ J Immunol, 2020, 205(8):2066-2076] PubMed: 32938730

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.