GW9662

GW9662 is a potent and selective PPARγ antagonist with an IC50 of 3.3 nM, showing 10 and 1000-fold selectivity over PPARα and PPARδ, respectively.

Product Specifications

CAS Number

[22978-25-2]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

PPAR

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage; Metabolic Enzyme/Protease; Vitamin D Related/Nuclear Receptor

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/GW9662.html

Purity

99.79

Solubility

DMSO : ≥ 100 mg/mL

Smiles

O=C(NC1=CC=CC=C1)C2=CC([N+]([O-])=O)=CC=C2Cl

Molecular Formula

C13H9ClN2O3

Molecular Weight

276.68

Precautions

H302, H315, H319, H335

References & Citations

[1]Leesnitzer LM, et al. Functional consequences of cysteine modification in the ligand binding sites of peroxisome proliferator activated receptors by GW9662. Biochemistry. 2002 May 28;41 (21) :6640-50.|[2]Seargent JM, et al. GW9662, a potent antagonist of PPARgamma, inhibits growth of breast tumor cells and promotes the anticancer effects of the PPARgamma agonist BRL 49653, independently of PPARgamma activation. Br J Pharmacol. 2004 Dec;143 (8) :933-7.|[3]Sato K, et al. PPARγ antagonist attenuates mouse immune-mediated bone marrow failure by inhibition of T cell function.Haematologica. 2016 Jan;101 (1) :57-67.|[4]Collino M, et al. The selective PPARgamma antagonist GW9662 reverses the protection of LPS in a model of renal ischemia-reperfusion. Kidney Int. 2005 Aug;68 (2) :529-36.