GW-9662

SKU: orb1305873

Description

GW9662 is a potent and selective PPARγ antagonist (IC50=3.3 nM) used to investigate metabolic and inflammatory disease mechanisms in research models. Its application extends to studying cancer biology, with demonstrated anti-tumor effects in both cellular and animal studies.

Research Area

Cardiovascular Research

Key Properties

• CAS Number: 22978-25-2
• MW: 276.68
• Purity: >98%
• Formula: C₁₃H₉ClN₂O₃
• SMILES: [O-][N+](=O)c1ccc(Cl)c(c1)C(=O)Nc1ccccc1
• Target: Transcription factor
• Solubility: Soluble in DMSO (up to 50 mg/ml) or in Ethanol (up to 10 mg/ml).

Bioactivity

• Target IC50:
  PPARγ:3.3 nM|PPARδ:2000 nM|PPARα:32 nM|MDA-MB-231 cells:20-30 µM|MDA-MB-468 cells:20-30 µM|MCF-7 cells:20-30 µM
• In Vivo:
  METHODS: To study the blocking effect of GW9662 on the protective effect of lipopolysaccharide, first, rats were pretreated with lipopolysaccharide (1 mg/kg,i.p.), which could significantly weaken all ischemia/reperfusion injury characteristics caused by renal injury and dysfunction. Then, GW9662 (1 mg/kg) was intraperitoneally injected into the rats. RESULTS: GW9662 can block the protective effect of lipopolysaccharide.
• In Vitro:
  METHODS: Human breast cancer cell lines (MCF7, MDA-MB-468, and MDA-MB-231) were treated with GW9662 (100 nM-50 mM) for 72 hours, and MTT assay was used to detect the inhibition of cell growth. RESULTS: GW9662 significantly inhibited the proliferation of MCF7, MDA-MB-468, and MDA-MB-231 cells (IC50= 20-30 μM).
• Cell Research:
  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.(Only for Reference)

Storage & Handling

• Storage: RT
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

inhibit, Inhibitor, GW 9662, GW9662, GW-9662, TIMTEC-BB SBB 006523, TIMTEC-BB SBB006523, TIMTEC-BB SBB-006523, PPARα, PPAR, Peroxisome proliferator-activated receptors, PPARδ, PPARγ

Compound Identifiers

PubChem CID

644213