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GW9662

Name: GW9662
Brand: Selleck Chemicals
SKU: S2915
Rating: 5 (50 reviews)

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.

CAS No. 22978-25-2

Selleck's GW9662 has been cited by 50 publications

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PPAR Signaling Pathway Map

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	NF;wRlhHfW6ldHnvckBie3OjeR?=		MYizNEBucW6\|		NGfnb4tCdnSjZ3;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=>	MoDwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzF{OUS5O\|QoRjNzMkm0PVc1RC:jPh?=

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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

References

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Solubility (25°C)

In vitro	DMSO	55 mg/mL (198.78 mM)
	Water	Insoluble
	Ethanol	Insoluble
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. Click to purchase: Corn Oil	9mg/mL

Chemical Information

Molecular Weight	276.68
Formula	C₁₃H₉ClN₂O₃
CAS No.	22978-25-2
Storage	3 years	-20°C	powder
Storage	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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Tech Support

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