Reagents and instruments for immunology, cell biology and molecular biology.

Fatostatin [125256-00-0]

Print

Cat# HY-14452-5mg

Size : 5mg

Brand : MedChemExpress

Request more information

Description

Fatostatin (125B11), a specific inhibitor of SREBP activation, impairs the activation of SREBP-1 and SREBP-2. Fatostatin binds to SCAP (SREBP cleavage-activating protein), and inhibits the ER-Golgi translocation of SREBPs. Fatostatin decreases the transcription of lipogenic genes in cells. Fatostatin possesses antitumor properties, and lowers hyperglycemia in ob/ob mice^[1]^[2].

Cellular Effect

Cell Line	Type	Value	Description	References
CHO-K1	IC₅₀	10 μM Compound: 1, 125B11	Inhibition of SREBP2 activation expressed in CHO-K1 cells by densitometric analysis Inhibition of SREBP2 activation expressed in CHO-K1 cells by densitometric analysis	[PMID: 21561152]
CHO-K1	IC₅₀	5.6 μM Compound: 1, 125B11	Inhibition of SREBP2 activation expressed in CHO-K1 cells co-transfected with pSRE-Luc plasmid assessed as inhibition of luciferase expression after 20 hrs by luciferase reporter gene assay Inhibition of SREBP2 activation expressed in CHO-K1 cells co-transfected with pSRE-Luc plasmid assessed as inhibition of luciferase expression after 20 hrs by luciferase reporter gene assay	[PMID: 21561152]

In Vitro

Fatostatin (125B11) (0.1-1 μM; 3 days) inhibits the androgen-independent prostate cancer cell proliferation (IC₅₀=0.1 μM) in an independent of the known IGF1-signaling pathway. Fatostatin inhibits insulin-induced adipogenesis of 3T3-L1 cells^[1].
Fatostatin directly binds SCAP and blocks its ER-to-Golgi transport with IC₅₀ of 2.5 and 10 μM in mammalian cells.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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

Fatostatin (125B11) (30 mg/kg; 150 μL; i.p. injection; daily for 28 days) reduces adiposity, ameliorated fatty liver by reducing triglyceride (TG) storage, and lowered hyperglycemia in ob/ob mice^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Four-to-five-week-old homozygous male obese (ob/ob) mice (C57BL/6J)^[2]
Dosage:	30 mg/kg; 150 μL
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.

Molecular Weight

294.41

Formula

C₁₈H₁₈N₂S

CAS No.

125256-00-0

Appearance

Solid

Color

White to yellow

SMILES

CCCC1=NC=CC(C2=NC(C3=CC=C(C)C=C3)=CS2)=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : ≥ 27 mg/mL (91.71 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.3966 mL	16.9831 mL	33.9662 mL
5 mM	0.6793 mL	3.3966 mL	6.7932 mL
10 mM	0.3397 mL	1.6983 mL	3.3966 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (8.49 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (8.49 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: 2.5 mg/mL (8.49 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: Corn Oil
Solubility: 5 mg/mL (16.98 mM); Suspended solution; Need ultrasonic

Purity & Documentation

Purity: 99.85%

Data Sheet (276 KB) SDS (396 KB)

COA (245 KB) HNMR (247 KB) LCMS (93 KB)

Handling Instructions (2659 KB)

References

[1]. Choi Y, et al. Identification of bioactive molecules by adipogenesis profiling of organic compounds. J Biol Chem. 2003 Feb 28;278(9):7320-4. [Content Brief]

[2]. Kamisuki S, et al. A small molecule that blocks fat synthesis by inhibiting the activation of SREBP. Chem Biol. 2009 Aug 28;16(8):882-92. [Content Brief]

[3]. Li X et al. Fatostatin displays high antitumor activity in prostate cancer by blocking SREBP-regulated metabolic pathways and androgen receptor signaling. Mol Cancer Ther. 2014 Apr;13(4):855-66. [Content Brief]

[4]. Shao W et al. Fatostatin blocks ER exit of SCAP but inhibits cell growth in a SCAP-independent manner. J Lipid Res. 2016 Aug;57(8):1564-73. [Content Brief]

[5]. Inoue K et al. Fatostatin, an SREBP inhibitor, prevented RANKL-induced bone loss by suppression of osteoclast differentiation. Biochim Biophys Acta. 2015 Nov;1852(11):2432-41. [Content Brief]

You might also be interested by the following products:

Cat#

Description

Cond.

Price Bef. VAT

AP02035SU-N

Homocysteine Rabbit Polyclonal Antibody

100ul

364018-200ul

LSR (Lipolysis Stimulated Lipoprotein Receptor, LISCH7, ILDR3, LISCH, Lipolysis-Stimulated Remnant, Immunoglobulin-Like Domain Containing Receptor 3)

200ul

NB-64-45602-5mg

Fatostatin [125256-00-0]

5mg

Fatostatin [125256-00-0]

Cat# HY-14452-5mg

Brand : MedChemExpress

Fatostatin Related Antibodies

You might also be interested by the following products: