M6191
GW9662
>98% (HPLC)
Sinônimo(s):
2-Chloro-5-nitro-N-phenylbenzamide
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About This Item
Fórmula empírica (Notação de Hill):
C13H9ClN2O3
Número CAS:
Peso molecular:
276.68
Número MDL:
Código UNSPSC:
51111800
ID de substância PubChem:
NACRES:
NA.77
Produtos recomendados
Ensaio
>98% (HPLC)
Formulário
powder
cor
white
solubilidade
DMSO: 26 mg/mL
H2O: insoluble
temperatura de armazenamento
2-8°C
cadeia de caracteres SMILES
[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)
chave InChI
DNTSIBUQMRRYIU-UHFFFAOYSA-N
Informações sobre genes
human ... PPARG(5468)
Aplicação
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.
Ações bioquímicas/fisiológicas
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.
GW9662 is an irreversible PPARγ antagonist; inhibits connective tissue growth factor, and activation of CD36 by IL-4.
Características e benefícios
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.
Informações legais
Sold for research purposes only, under agreement from GlaxoSmithKline
Código de classe de armazenamento
11 - Combustible Solids
Classe de risco de água (WGK)
WGK 3
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PPAR Research, 2017(43), 26303-26313 (2017)
Functional consequences of cysteine modification in the ligand binding sites of peroxisome proliferator activated receptors by GW9662
Leesnitzer LM, et al.
Biochemistry, 41(21), 6640-6650 (2002)
The synergistic enhancement of cloning efficiency in individualized human pluripotent stem cells by peroxisome proliferative-activated receptor-gamma (PPARgamma) activation and rho-associated kinase (ROCK) inhibition
Kajabadi NS, et al.
The Journal of Biological Chemistry, 290(43), 26303-26313 (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
Seargent JM, et al.
British Journal of Pharmacology, 143(8), 933-937 (2004)
Efstathia Papageorgiou et al.
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
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