Fatostatin (Synonyms: 125B11) |
Catalog No.GC36031
One-Click Copy Product Info
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Fatostatin (125B11) is a specific inhibitor of sterol regulatory element-binding proteins (SREBP) activation, inhibiting the activation of both SREBP-1 and SREBP-2.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 125256-00-0
Sample solution is provided at 25 µL, 10mM.
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Fatostatin (125B11) is a specific inhibitor of sterol regulatory element-binding proteins (SREBP) activation, inhibiting the activation of both SREBP-1 and SREBP-2[1]. Fatostatin blocks the occurrence of SCAP (SREBP cleavage-activating protein), preventing the transport of SREBP to the Golgi for activation, thereby reducing the transcription of genes involved in lipid and cholesterol biosynthesis[2]. Fatostatin can inhibit the AKT/mTORC1/GPX4 signaling pathway, inducing ferroptosis[3].
In vitro, Fatostatin (5μM) treatment of U87, T98G, MDA-MB-453, and Jurkat T cells for 24 or 48 hours induced spindle damage and mitotic arrest, causing all cells to be inhibited in the G2/M phase[4]. Fatostatin (0-20 μM) treatment of CHO cells dose-dependently inhibited the expression of HMG-CoA synthase (HMGCS 1), blocking intracellular SREBP processing[5].
In vivo, Fatostatin (15 mg/kg) administered via intraperitoneal injection for 42 days significantly inhibited tumor growth in mice with subcutaneous C4-2B tumor implants, reducing the proliferation index (Ki67 status), serum prostate-specific antigen (PSA) levels, and mRNA and protein levels of SREBP downstream genes in tumor cells[6]. Fatostatin (30 mg/kg) administered via intraperitoneal injection for 28 days in obese ob/ob mice blocked the increase in body weight, blood glucose, and liver fat accumulation[7].
References:
[1] Ma X, Zhao T, Yan H, et al. Fatostatin reverses progesterone resistance by inhibiting the SREBP1-NF-κB pathway in endometrial carcinoma[J]. Cell Death & Disease, 2021, 12(6): 544.
[2] Lee S H, Lee J H, Im S S. The cellular function of SCAP in metabolic signaling[J]. Experimental & molecular medicine, 2020, 52(5): 724-729.
[3] Cai J, Ye Z, Hu Y, et al. Fatostatin induces ferroptosis through inhibition of the AKT/mTORC1/GPX4 signaling pathway in glioblastoma[J]. Cell Death & Disease, 2023, 14(3): 211.
[4] Gholkar A A, Cheung K, Williams K J, et al. Fatostatin inhibits cancer cell proliferation by affecting mitotic microtubule spindle assembly and cell division[J]. Journal of Biological Chemistry, 2016, 291(33): 17001-17008.
[5] Shao W, Machamer C E, Espenshade P J. Fatostatin blocks ER exit of SCAP but inhibits cell growth in a SCAP-independent manner[J]. Journal of lipid research, 2016, 57(8): 1564-1573.
[6] Li X, Chen Y T, Hu P, et al. Fatostatin displays high antitumor activity in prostate cancer by blocking SREBP-regulated metabolic pathways and androgen receptor signaling[J]. Molecular cancer therapeutics, 2014, 13(4): 855-866.
[7] Kamisuki S, Mao Q, Abu-Elheiga L, et al. A small molecule that blocks fat synthesis by inhibiting the activation of SREBP[J]. Chemistry & biology, 2009, 16(8): 882-892.
Cell experiment [1]: | |
Cell lines | U87, T98G, MDA-MB-453, and Jurkat T-cells |
Preparation method | U87, T98G, MDA-MB-453, and Jurkat T-cells treated with DMSO or 5μM Fatostatin for 24h (U87 cells were treated for 48 h). |
Reaction Conditions | 5μM; 24、48h |
Applications | Fatostatin arrested all cell lines in G2/M. |
Animal experiment [2]: | |
Animal models | Athymic nu/nu male mice |
Preparation method | Athymic nu/nu male mice were implanted subcutaneously with C4-2B cells. Mice bearing C4-2B tumors with a mean volume of 100 mm3 were randomly divided into vehicle control (sterile PBS) or Fatostatin (15mg/kg) groups with intraperitoneal injection for 42 days. |
Dosage form | 15mg/kg; i.p. |
Applications | Fatostatin significantly inhibited subcutaneous C4-2B tumor growth and markedly decreased serum prostate-specific antigen (PSA) level compared with the control group. |
References: | |
| Cas No. | 125256-00-0 | SDF | |
| Synonyms | 125B11 | ||
| Canonical SMILES | CCCC1=NC=CC(C2=NC(C3=CC=C(C)C=C3)=CS2)=C1 | ||
| Formula | C18H18N2S | M.Wt | 294.41 |
| Solubility | DMSO: ≥ 27 mg/mL (91.71 mM); Water: < 0.1 mg/mL (insoluble) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.3966 mL | 16.9831 mL | 33.9662 mL |
| 5 mM | 679.3 μL | 3.3966 mL | 6.7932 mL |
| 10 mM | 339.7 μL | 1.6983 mL | 3.3966 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 3 reference(s) in Google Scholar.)