Name: Fatostatin HBr
Brand: Selleck Chemicals
SKU: S8284
Availability: InStock
Rating: 5 (15 reviews)

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Quality Control

Batch: Purity: 99.71%

99.71

Related Targets	Dehydrogenase HSP Transferase P450 (e.g. CYP17) PDE phosphatase PPAR Vitamin Carbohydrate Metabolism Mitochondrial Metabolism
Other SREBP Inhibitors	Cinobufotalin

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description	PMID
CHO-K1 cells	Function assay		20 h	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, IC50=5.6 μM	21561152
mouse hepatocytes	Function assay	1 uM	90 mins	Metabolic stability in mouse hepatocytes at 1 uM after 90 mins by LC-MS/MS analysis	21561152
InhA cells	Antimicrobial assay			Antimicrobial activity against Mycobacterium tuberculosis H37Rv over-expressing InhA cells assessed as upshift of MIC relative to wild type	24967731
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

Ethanol : 58 mg/mL

DMSO : 7 mg/mL (18.65 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
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.
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.
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.
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 Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	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.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

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.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

+

%

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 ddH₂O, 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.

Chemical Information, Storage & Stability

Molecular Weight	375.33	Formula	C₁₈H₁₈N₂S·HBr	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	298197-04-3	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	125B11 HBr			Smiles	CCCC1=NC=CC(=C1)C2=NC(=CS2)C3=CC=C(C=C3)C.Br

Mechanism of Action

Targets/IC₅₀/Ki	SREBPs
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. 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.
In vivo	Fatostatin blocks increases in body weight, blood glucose, and hepatic fat accumulation in obese ob/ob mice, even under uncontrolled food intake. Fatostatin significantly inhibits subcutaneous C4-2B tumor growth and markedly decreases serum PSA level compared to the control group.
References	[1] https://pubmed.ncbi.nlm.nih.gov/19716478/ [2] https://pubmed.ncbi.nlm.nih.gov/24493696/

Applications

Methods	Biomarkers	PMID
Western blot	p-SREBP-1 / N-SREBP-1 / p-SREBP-2 / N-SREBP-2 / FASN / HMGCR AR / PSA Cyclin B / PH3	24493696
Immunofluorescence	α-tubulin / centromere	27378817
Growth inhibition assay	Cell viability	24493696