GW9662

Catalog No.S2915

For research use only.

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.

GW9662 Chemical Structure

CAS No. 22978-25-2

Selleck's GW9662 has been cited by 54 publications

Purity & Quality Control

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Biological Activity

Description 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.
Targets
PPARγ [1]
(Cell-free assay)
PPARα [1]
(Cell-free assay)
3.3 nM 32 nM
In vitro

GW9662 binds to Cys(285) on PPARgamma which is conserved among all three PPARs. GW9662 acts as an antagonist of PPARgamma which is confirmed in an assay of adipocyte differentiation inhibition. [1] GW9662 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 GW9662 or growth-inhibitory mechanisms independent of PPARγ. Co-treatment with both Rosiglitazone (50 μM) and GW9662 (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 GW 9662 (2 μM). GW 9662 (2 μM) blocks IL-4 suppression of osteoclast formation in BMs. GW 9662 (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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
293H MVPGeY5kfGmxbjDhd5NigQ>? NUnSd5pqOzBibXnudy=> NHHLPHpCdnSjZ3;ubZN1KGGldHn2bZR6KGG2IHj1cYFvKFCSQWLnZY1u[SCneIDy[ZN{\WRiaX6gNlk{UCClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25iaX6gdo9{cWeuaYThfo9v\S2rbnT1Z4VlKHS{YX7zZ5JqeHSrb37hcEBz\XOyb37z[UBxemWrbnP1ZoF1\WRiZn;yJFMxKG2rboOg[o9tdG:5ZXSgZpkhem:|aXfsbZRigm:wZTDh[IRqfGmxbjDhcoQhdWWjc4Xy[YQh[W[2ZYKgNVYhcHK|IHL5JJJmeG:{dHXyJIdmdmVvYnHz[YQhTlKHVDDhd5NigSxiRVO1NF0xNjByMt88US=> MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{OTJ7NEm3OEc,OzF{OUS5O|Q9N2F-
Assay
Methods Test Index PMID
Western blot Vimentin / Slug / MMP9 / MMP2 30912275
Growth inhibition assay Cell proliferation 30912275
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, GW9662 (1 mg/kg i.p.) abolishes the protective effects of LPS. [5]

Protocol (from reference)

Kinase Assay:[2]
  • Binding 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).

Cell Research:[1]
  • Cell lines: MDA-MB-231 cells
  • Concentrations: 10 μM
  • Incubation Time: 10 days
  • Method: MDA-MB-231 cells are seeded at a density of 1 × 105 cells per 25 cm3 tissue culture flask. After 24 h (day 0), the growth medium is replaced with fresh medium containing rosiglitazone (50 μM), GW9662 (10 μM) or both together. Control flasks receives 0.1% DMSO. Cells are harvested on days 0, 3, 5, 7, 10 for each treatment condition by trypsinisation, stained using trypan blue, and the total and viable number of cells per flask calculates using a haemocytometer.
Animal Research:[5]
  • Animal Models: male Wistar rats
  • Dosages: 1 mg/kg
  • Administration: intraperitoneal injection

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
5% DMSO+corn oil
For best results, use promptly after mixing.

9mg/mL

Chemical Information

Molecular Weight 276.68
Formula

C13H9ClN2O3

CAS No. 22978-25-2
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1=CC=C(C=C1)NC(=O)C2=C(C=CC(=C2)[N+](=O)[O-])Cl

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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