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GW9662 PPARγ Antagonist

Name: GW9662
SKU: S2915
Availability: InStock
Rating: 5 (80 reviews)

Cat.No.S2915

GW9662 is a selective PPAR antagonist for PPARγ with IC50 of 3.3 nM in a cell-free assay, with at least 10- to 600-fold functional selectivity in cells with PPARγ versus PPARα and PPARδ.

Chemical Structure

Molecular Weight: 276.68

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.94%

99.94

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Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID
293H	Function assay		30 mins		Antagonist activity at human PPARgamma expressed in 293H cells assessed as reduction in transcriptional response preincubated for 30 mins followed by addition and measured after 16 hrs by reporter gene-based FRET assay, EC50=0.002μM	31294974
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	276.68	Formula	C₁₃H₉ClN₂O₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	22978-25-2	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	C1=CC=C(C=C1)NC(=O)C2=C(C=CC(=C2)[N+](=O)[O-])Cl

Solubility

In vitro
Batch:

DMSO : 55 mg/mL (198.78 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

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 Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	9.000mg/ml (32.53mM)	Taking the 1 mL working solution as an example, add 50 μL of 180 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.
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.	0.150mg/ml (0.54mM)	Taking the 1 mL working solution as an example, add 50 μL of 3 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.
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.

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.

Mechanism of Action

Targets/IC₅₀/Ki	PPARγ ^[1] (Cell-free assay) 3.3 nM PPARα ^[1] (Cell-free assay) 32 nM
In vitro	GW9662 binds to Cys(285) on PPARgamma which is conserved among all three PPARs. This compound acts as an antagonist of PPARgamma which is confirmed in an assay of adipocyte differentiation inhibition. ^[1] It prevents activation of PPARγ and inhibits growth of human mammary tumour cell lines (MCF7, MDA-MB-468, MDA-MB-231) with IC50 of 20 μM-30 μM, suggesting either the existence of PPARγ agonistic properties of this chemical or growth-inhibitory mechanisms independent of PPARγ. Co-treatment with this compound (10 μM) results in statistically lower viable cell numbers after 7 days in MDA-MB-231 cells. ^[2] PPARγ1 ligands could suppress RANKL-induced osteoclast formation in primary murine myeloid (BMs) and RAW264.7 cells. Importantly, suppression by these ligands is reversed in a concentration-dependent fashion with this chemical (2 μM). It (2 μM) blocks IL-4 suppression of osteoclast formation in BMs. This compound (1 μM) blocks RANKL activation of NF-κB in RAW264.7 cells. ^[3] GW9662 (10 μM) inhibits hormone- and agonist-induced adipogenesis of primary preadipocytes from patients with thyroid eye disease. ^[4]
Kinase Assay	Binding assay
Kinase Assay	The human PPARα, PPARγ, and PPARδ ligand binding domains (LBDs) are expressed in E. coli as polyhistidine-tagged fusion proteins. Receptors are immobilized on SPA beads by addition of the desired receptor (15 nM) to a slurry of streptavidin-modifed SPA beads (0.5 mg/mL) in assay buffer. The mixture is allowed to equilibrate for at least 1 hour at room temperature, and the beads are pelleted by centrifugation at 1×10³ g. The supernate is discarded, and the beads are resuspended in the original volume of fresh assay buffer with gentle mixing. The centrifugation/resuspension procedure is repeated, and the resulting slurry of receptor-coated beads is used immediately or stored at 4 ℃ for up to 1 week before use. [3H]GW2443 are used as radioligands for determination of competition binding to PPARα, PPARγ, and PPARδ, respectively. Unless otherwise indicated, the buffer used for all assays is 50 mM HEPES (pH 7), 50 mM NaCl, 5 mM CHAPS, 0.1 mg/mL BSA, and 10 mM DTT. For some experiments, the HEPES (pH 7) is replaced with 50 mM Tris (pH 8).
In vivo	Pretreatment with LPS (1 mg/kg i.p.) significantly attenuates all markers of renal injury and dysfunction caused by ischemia/reperfusion (I/R) injury in rats. Most notably, this compound (1 mg/kg i.p.) abolishes the protective effects of LPS. ^[5]
References	[1] https://pubmed.ncbi.nlm.nih.gov/12022867/ [2] https://pubmed.ncbi.nlm.nih.gov/15533890/ [3] https://pubmed.ncbi.nlm.nih.gov/11226258/ [4] https://pubmed.ncbi.nlm.nih.gov/12519830/ [5] https://pubmed.ncbi.nlm.nih.gov/16014029/

Applications

Methods	Biomarkers	Images	PMID
Western blot	Vimentin / Slug / MMP9 / MMP2		30912275
Growth inhibition assay	Cell proliferation		30912275

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