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CAS No.: 22978-25-2

GW9662 Catalog No. CSN11131

Synonyms: TIMTEC-BB SBB006523;TIMTEC-BB;SBB006523

GW9662 selectively antagonizes PPARγ with IC50 of 3.3 nM. It can inhibit the growth of mammary cancer cells.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 PPARγ

IC50:3.3nM
描述GW9662 is a selective and irreversible PPARγ antagonist with IC50 value of 5.4nM, 10- and 600-fold selectivity against PPARα and PPARδ with IC50 values of 39nM and 1.2μM, respectively. GW9662 had no effect on the ability of any of the PPARs to form heterodimers with RXR. GW9662 could dose-dependently antagonize PPARγ-GAL4-mediated transcription induced by rosiglitazone with IC50 value of 7.6nM. Consistent with this, rosiglitazone-induced increases in aP2 and Oil Red O staining could be completely blocked in C3H10T1/2 cells treated with 1μM GW9662, suggesting the anti-adipogenesis function of GW9662^[1]. GW9662 within 2μM clearly blocked the ability of IL-4 (0.1, 0.5ng/ml, but not 1ng/ml) to suppress RANKL/M-CSF-induced osteoclastogenesis in bone marrow monocytes through inhibition of PPARγ1^[2]. GW 9662 at concentration of 1μM could antagonize the potentiation of HL-60 cell differentiation induced by PGD2, PGJ2, indomethacin and MPA post 4 days^[3].
作用机制GW9662 exhibited a competition binding assay against the human ligand binding domain and covalently modified Cys of PPARγ.^[1]
动物研究
剂量
Mice: 5 mg/kg^[4] (i.p.), 10 mg/kg^[5] (i.p.)

给药途径
i.p.
参考文献

动物研究
剂量	Mice: 5 mg/kg^[4] (i.p.), 10 mg/kg^[5] (i.p.)
给药途径	i.p.

[1] Leesnitzer LM, Parks DJ, 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] Bendixen AC, Shevde NK, et al. IL-4 inhibits osteoclast formation through a direct action on osteoclast precursors via peroxisome proliferator-activated receptor gamma 1. Proc Natl Acad Sci U S A. 2001 Feb 27;98(5):2443-8. Epub 2001 Feb 20.
[3] Desmond JC, Mountford JC, et al. The aldo-keto reductase AKR1C3 is a novel suppressor of cell differentiation that provides a plausible target for the non-cyclooxygenase-dependent antineoplastic actions of nonsteroidal anti-inflammatory drugs. Cancer Res. 2003 Jan 15;63(2):505-12.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.6143 mL
- 18.0717 mL
- 36.1435 mL
- 5 mM
- 0.7229 mL
- 3.6143 mL
- 7.2287 mL
- 10 mM
- 0.3614 mL
- 1.8072 mL
- 3.6143 mL

技术信息

CAS号

22978-25-2

储存条件

粉末: Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C13H9ClN2O3

运输

蓝冰

分子量

276.68

别名

TIMTEC-BB SBB006523;TIMTEC-BB;SBB006523

溶解度

DMSO	55.0 mg/mL (198.8 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

5% DMSO+corn oil

9 mg/mL

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GW9662 Catalog No. CSN11131

靶点选择性

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