| 名稱 | LY2409881 trihydrochloride |
| 描述 | LY2409881 trihydrochloride is a novel specific inhibitor of IKK2 (IC50: 30 nM); IC50 for IKK1 and other common kinases is at least one log higher. |
| 細(xì)胞實(shí)驗(yàn) | Cytotoxicity is evaluated using the CellTiter-Glo Reagent according to the manufacturer's manual. Experiments are carried out in 96-well plates, with each treatment in triplicate. Samples are taken at typically 24, 48, and 72 hours after treatment. Cytotoxicity is expressed by the decreasing percentage of live cells in each treatment relative to the untreated control from the same experiment. IC50 for each cell line is calculated using the CalcuSyn Version 2.0 software.(Only for Reference) |
| 激酶實(shí)驗(yàn) | CYP3A activity is assessed using the probe reactions, midazolam-1′-hydroxylation and testosterone 6β-hydroxylation. For reversible inhibition, incubations (37°C, 10 min) are composed of (final concentrations): potassium phosphate buffer (100 mM, pH 7.4), β-NADPH (1 mM), magnesium chloride (5 mM), microsomal protein (0.025 mg/mL), probe substrate (1 μM midazolam or 25 μM testosterone), LCL161 (0, 0.5, 1, 5, 10, 25, 50, or 100 μM) and organic solvent (0.2% acetonitrile for midazolam, 0.2% methanol for testosterone). After a 3-minute preincubation, the reactions are initiated by addition of β-NADPH and terminated by addition of acetonitrile (two volumes). Reactions are previously shown to be linear with respect to time and protein concentration (results not shown) with midazolam and testosterone turnover of 8.7±1.3% (n=3) and 2.6±0.20%, respectively. Formation of 1′-hydroxymidazolam and 6β-hydroxytestosterone is determined by LC-MS/MS as described below[3]. |
| 體外活性 | 在SCID-beige移植瘤小鼠模型中,LY2409881（50/100/200 mg/kg,i.p.）可顯著抑制腫瘤生長(zhǎng). |
| 體內(nèi)活性 | LY240988對(duì)卵巢癌SKOV3細(xì)胞株具有中等毒性。在彌漫性大B細(xì)胞淋巴瘤細(xì)胞中,LY2409881對(duì)激活的NF-?B有抑制作用,濃度和時(shí)間依賴性地抑制細(xì)胞生長(zhǎng)并使細(xì)胞凋亡。在SUDHL2細(xì)胞中,LY2409881可協(xié)同環(huán)磷酰胺和阿霉素抑制細(xì)胞生長(zhǎng),但對(duì)LY1細(xì)胞無(wú)協(xié)同效果。在SUDHL22和LY1細(xì)胞中,組蛋白去乙?；敢种苿┝_米地辛與LY2409881可協(xié)同抑制細(xì)胞生長(zhǎng)。 |
| 存儲(chǔ)條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 16 mg/mL (26.9 mM)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
H2O : < 1 mg/mL (insoluble or slightly soluble)
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| 關(guān)鍵字 | LY 2409881 | LY2409881 trihydrochloride | LY-2409881 Trihydrochloride | LY2409881 Trihydrochloride | Inhibitor | IκB kinase | Apoptosis | IKK | LY-2409881 | inhibit | I kappa B kinase | LY-2409881 trihydrochloride | LY 2409881 Trihydrochloride |
| 相關(guān)產(chǎn)品 | Lidocaine hydrochloride | Metronidazole | 5-Fluorouracil | Stavudine | Tributyrin | Dextran sulfate sodium salt (MW 4500-5500) | Myricetin | Sorafenib | L-Ascorbic acid | Acetylcysteine | Sodium 4-phenylbutyrate | Kaempferol |
| 相關(guān)庫(kù) | 抑制劑庫(kù) | 抗乳腺癌化合物庫(kù) | 經(jīng)典已知活性庫(kù) | 已知活性化合物庫(kù) | 激酶抑制劑庫(kù) | 抗衰老化合物庫(kù) | HIF-1化合物庫(kù) | 抗卵巢癌化合物庫(kù) | NF-κB 通路分子庫(kù) | 抗前列腺癌化合物庫(kù) |