추천 제품
분석
>98% (HPLC)
양식
powder
색상
white
solubility
DMSO: 26 mg/mL
H2O: insoluble
저장 온도
2-8°C
SMILES string
[O-][N+](=O)c1ccc(Cl)c(c1)C(=O)Nc2ccccc2
InChI
1S/C13H9ClN2O3/c14-12-7-6-10(16(18)19)8-11(12)13(17)15-9-4-2-1-3-5-9/h1-8H,(H,15,17)
InChI key
DNTSIBUQMRRYIU-UHFFFAOYSA-N
유전자 정보
human ... PPARG(5468)
애플리케이션
GW9662 has been used as a peroxisome proliferator activated receptor γ (PPARγ) antagonist in human pluripotent stem cells, in phenylephrine stimulated cardiomyocytes and to inhibit the protective effect of telmisartan pheochromocytoma, PC12 cells.
생화학적/생리학적 작용
GW9662 (2-chloro-5-nitrobenzanilide) binds to the ligand binding site of the peroxisome proliferator activated receptor γ (PPARγ) and results in the inhibition of adipocyte differentiation. It favors cell growth suppression in breast cancer cell lines even in the presence of PPARγ agonist rosiglitazone. It stimulates M2c macrophages differentiation and triggers growth arrest-specific 6 (Gas6) expression. GW9662 co treatment with other PPARγ ligands elicits antiproliferative effects on the glioblastoma stem cells and could be a potent therapeutic agent.
GW9662 is an irreversible PPARγ antagonist. GW9662 inhibits connective tissue growth factor and activation of CD36 by IL-4.
특징 및 장점
This compound is featured on the Nuclear Receptors (PPARs) page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
법적 정보
Sold for research purposes only, under agreement from GlaxoSmithKline
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
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시험 성적서(COA)
이미 열람한 고객
Molecular medicine (Cambridge, Mass.), 14(7-8), 403-411 (2008-05-14)
PPARgamma, a member of the peroxisome proliferator-activated receptor family, is overexpressed in prostate cancer. Natural and synthetic ligands of PPARgamma via genomic and nongenomic actions promote cell cycle arrest and apoptosis of several prostate cancer cells, in vitro. Insulin-like growth
The PPAR-gamma antagonist GW9662 elicits differentiation of M2c-like cells and upregulation of the MerTK/Gas6 axis: a key role for PPAR-gamma in human macrophage polarization
Journal of Inflammation, 12(1), 36-36 (2015)
GW9662, a potent antagonist of PPARgamma, inhibits growth of breast tumour cells and promotes the anticancer effects of the PPARgamma agonist rosiglitazone, independently of PPARgamma activation
British Journal of Pharmacology, 143(8), 933-937 (2004)
Combination Treatment with PPARgamma Ligand and Its Specific Inhibitor GW9662 Downregulates BIS and 14-3-3 Gamma, Inhibiting Stem-Like Properties in Glioblastoma Cells
BioMed Research International, 2017(1), 36-36 (2017)
Bezafibrate attenuates pressure overload-induced cardiac hypertrophy and fibrosis
PPAR Research, 2017(43), 26303-26313 (2017)
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