Name: FH535
Brand: Selleck Chemicals
SKU: S7484
Availability: InStock
Rating: 5 (20 reviews)

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Batch: S748401 DMSO]72 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 100.00%

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COA
NMR
HPLC
SDS
Datasheet

100.00

Related Targets	JAK TGF-beta/Smad ERK GSK-3 ROCK Hedgehog/Smoothened PKA Secretase STAT Casein Kinase
Other Wnt/beta-catenin Inhibitors	ICG-001 IWR-1-endo IWP-2 Isoquercitrin Tegatrabetan (BC-2059) SKL2001 BML-284 (Wnt agonist 1) PRI-724 (Foscenvivint) Salinomycin (from Streptomyces albus) PNU-74654

Solubility

In vitro
Batch:

DMSO : 72 mg/mL (199.33 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : 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.
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.	1.8mg/ml (4.98mM)	Taking the 1 mL working solution as an example, add 50 μL of 36 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.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.36mg/ml (1.00mM)	Taking the 1 mL working solution as an example, add 50 μL of 7.2 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. 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	361.20	Formula	C₁₃H₁₀Cl₂N₂O₄S	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	108409-83-2	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CC1=C(C=CC(=C1)[N+](=O)[O-])NS(=O)(=O)C2=C(C=CC(=C2)Cl)Cl

Mechanism of Action

Targets/IC₅₀/Ki	Wnt/β-catenin PPARγ PPARδ
In vitro	FH535 antagonizes β-Catenin/Tcf–mediated transcription, and inhibits recruitment of the coactivators GRIP1 and β-catenin to PPARδ and PPARγ. This compound shows selective anti-proliferation effect on some cancer cells expressing high or active Wnt/β-catenin pathway. It increases cigarette smoke condensate cytotoxicity, and causes changes in β-catenin and EGR-1 signaling. This chemical has potential therapeutic value in treatment of liver cancer by targeting liver cancer stem cells and hepatocellular carcinoma cell lines.
Kinase Assay	High-throughput Library Screen
Kinase Assay	Three copies of the optimized or mutated Tcf-binding element from TOPFLASH or FOPFLASH driving a secreted alkaline phosphatase reporter gene are cloned into pCEP4 plasmid, replacing the cytomegalovirus promoter. The plasmids are transfected into HepG2 cells, and hygromycin-resistant clones are pooled. Library screening is done at 20 μmol/L concentration of this compound in HepG2 serum-free media. Hits are tested in the HCT116 cell line for inhibition of TOPFLASH luciferase activity but not for inhibition of a reporter activity controlled from β-actin promoter.
References	[1] https://pubmed.ncbi.nlm.nih.gov/18347139/ [2] https://pubmed.ncbi.nlm.nih.gov/22713211/ [3] https://pubmed.ncbi.nlm.nih.gov/24940873/

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FH535 Wnt/beta-catenin inhibitor

Chemical Structure

Molecular Weight: 361.20