| Field | Specification |
|---|---|
| Alternative names | 125B11 hydrobromide |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C18H19BrN2S |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
Fatostatin hydrobromide, also known as 125B11 hydrobromide, specifically inhibits SREBP activation and impairs activation of both SREBP-1 and SREBP-2. It binds SCAP (SREBP cleavage-activating protein) and blocks the ER-Golgi translocation of SREBPs, thereby reducing transcription of lipogenic genes in cells. The compound has antitumor properties and lowers hyperglycemia in ob/ob mice[1][2]. It is supplied as a light yellow to yellow solid (C18H19BrN2S, MW 375.33) at 99.52% purity.
Physical & Chemical Properties
| CAS Number | 298197-04-3 |
|---|---|
| Molecular Formula | C18H19BrN2S |
| Molecular Weight | 375.33 g/mol |
| Purity | 99.52% |
| Appearance | Solid |
| Color | Light yellow to yellow |
| SMILES | CCCC1=NC=CC(C2=NC(C3=CC=C(C)C=C3)=CS2)=C1.[H]Br |
| Signaling Pathway | Metabolic Enzyme/Protease |
| Solubility | In Vitro: DMSO: 25 mg/mL (66.61 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | 4°C, sealed storage, away from moisture. In solvent: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 25 mg/mL (66.61 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); sealed storage, away from moisture; avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 2.08 mg/mL (5.54 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.08 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (20.8 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 2
| Composition | 10% DMSO + 90% (20% SBE-β-CD in saline) |
|---|---|
| Result | 1 mg/mL (2.66 mM); suspension; requires sonication |
| How to prepare | Gives a suspension at 1 mg/mL. The suspension is suitable for oral and intraperitoneal dosing. For 1 mL of working solution: add 100 μL DMSO stock (10.0 mg/mL) to 900 μL 20% SBE-β-CD in saline. 20% SBE-β-CD in saline: dissolve 2 g SBE-β-CD powder in 10 mL saline until clear (4°C, store up to one week). |
Data provided by the manufacturer.
In Vitro
Fatostatin hydrobromide (125B11 hydrobromide) (0.1-1 μM; 3 days) suppresses proliferation of androgen-independent prostate cancer cells (IC50=0.1 μM), independent of the known IGF1-signaling pathway. Fatostatin hydrobromide also blocks insulin-induced adipogenesis in 3T3-L1 cells[1].
Cell Proliferation Assay[1]
| Cell Line | DU-145 cells |
|---|---|
| Concentration | 0.1, 1 μM |
| Incubation Time | 3 days |
| Result | Impaired the IGF1-induced growth at an IC50 of 0.1 μM. |
In Vivo
Daily i.p. dosing of Fatostatin hydrobromide (125B11 hydrobromide) at 30 mg/kg (150 mL) for 28 days lowers adiposity, improves fatty liver by decreasing triglyceride (TG) storage, and reduces hyperglycemia in ob/ob mice[2].
| Animal Model | Four-to-five-week-old homozygous male obese (ob/ob) mice (C57BL/6J)[2] |
|---|---|
| Dosage | 30 mg/kg; 150 mL |
| Administration | i.p. injection; daily for 28 days |
| Result | Blocked increases in body weight, blood glucose, and hepatic fat accumulation in obese ob/ob mice, even under uncontrolled food intake. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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