| 名稱 | GW9662 |
| 描述 | GW9662 (TIMTEC-BB SBB006523) is a PPARγ antagonist (IC50=3.3 nM) with selectivity. GW9662 can be used to study the pathogenesis of metabolic diseases, such as obesity and diabetes, by inhibiting the activity of PPARγ. GW9662 can be used to study the pathogenesis of inflammatory diseases, such as atherosclerosis and rheumatoid arthritis. GW9662 has anti-tumor effect. |
| 細(xì)胞實(shí)驗(yàn) | 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) |
| 激酶實(shí)驗(yàn) | Binding assay: The human PPARα, PPARγ, and PPARδ ligand binding domains (LBDs) are expressed in E. coli as polyhistidine-tagged fusion proteins. Receptors are immobilized on SPA beads by addition of the desired receptor (15 nM) to a slurry of streptavidin-modifed SPA beads (0.5 mg/mL) in assay buffer. The mixture is allowed to equilibrate for at least 1 hour at room temperature, and the beads are pelleted by centrifugation at 1×103 g. The supernate is discarded, and the beads are resuspended in the original volume of fresh assay buffer with gentle mixing. The centrifugation/resuspension procedure is repeated, and the resulting slurry of receptor-coated beads is used immediately or stored at 4 ℃ for up to 1 week before use. [3H]GW2443 are used as radioligands for determination of competition binding to PPARα, PPARγ, and PPARδ, respectively. Unless otherwise indicated, the buffer used for all assays is 50 mM HEPES (pH 7), 50 mM NaCl, 5 mM CHAPS, 0.1 mg/mL BSA, and 10 mM DTT. For some experiments, the HEPES (pH 7) is replaced with 50 mM Tris (pH 8). |
| 體外活性 | 方法：人乳腺癌腫瘤細(xì)胞系 （MCF7、 MDA-MB-468,、MDA-MB-231）用GW9662（(100 nM-50 mM）處理72小時(shí)，使用MTT實(shí)驗(yàn)檢測(cè)細(xì)胞生長(zhǎng)抑制情況。
結(jié)果：GW9662抑制MCF7、 MDA-MB-468,、MDA-MB-231細(xì)胞生長(zhǎng) （IC50=20 -30 μM）。[1] |
| 體內(nèi)活性 | 方法：為研究GW9662對(duì)脂多糖保護(hù)作用的阻斷作用，首先大鼠經(jīng)脂多糖（1 mg/kg,i.p.）預(yù)處理,可明顯減弱腎損傷和功能障礙引起的所有缺血/再灌注損傷特征，再將GW9662（1 mg/kg）腹腔注射給大鼠。
結(jié)果：GW9662可阻斷脂多糖的保護(hù)作用。[2] |
| 存儲(chǔ)條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | DMSO : 255 mg/mL (921.64 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 5 mg/mL (18.07 mM), Sonication is recommended.
Ethanol : 6.9 mg/mL (24.94 mM), Heating is recommended.
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| 關(guān)鍵字 | TIMTEC-BB SBB-006523 | TIMTEC-BB SBB 006523 | PPARδ | PPARγ | PPARα | PPAR | Peroxisome proliferator-activated receptors | Inhibitor | inhibit | GW-9662 | GW9662 |
| 相關(guān)產(chǎn)品 | Icariin | Daidzein | PHYTOL | Rosiglitazone | 5-Aminosalicylic Acid | Fenofibrate | Retinoic acid | 2,3-Butanediol | Cloxiquine | NPC 15199 | Naringenin | Maltitol |
| 相關(guān)庫(kù) | 抑制劑庫(kù) | 經(jīng)典已知活性庫(kù) | 已知活性化合物庫(kù) | 抗胰腺癌化合物庫(kù) | 抗糖尿病庫(kù) | 抗衰老化合物庫(kù) | NO PAINS 化合物庫(kù) | 抗高血壓化合物庫(kù) | 核受體化合物庫(kù) | 抗肥胖化合物庫(kù) | 神經(jīng)退行性疾病化合物庫(kù) | 表型篩選靶點(diǎn)鑒定庫(kù) |