| 名稱 | Bay 11-7085 |
| 描述 | Bay 11-7085 can irreversibly inhibit the IκBα phosphorylation induced by TNFα (IC50: 10 μM). |
| 細胞實驗 | Human umbilical vein endothelial cells (HUVEC) are isolated and maintained in culture. Cell toxicity is assessed by morphology and by MTT assay.(Only for Reference) |
| 激酶實驗 | In Gel Kinase Assay: In gel kinase assay for the proteins that phosphorylate IκB-α is carried out as detailed below. Whole cell extracts are prepared from HUVEC treated with TNFα (100 units/ml) for 15 min in the presence or absence of inhibitor (20 μM, pretreatment for 1 h) as indicated. Proteins are separated on a 10% SDS gel containing 0.5 mg/ml HIS-IκB-α. Gels are washed two times in 20% propanol, 50 mM Hepes, pH 7.6, for 30 min and two times in buffer A (50 mM Hepes, pH 7.6, 5 mM 2-mercaptoethanol) for 30 min, followed by a 1-h incubation with buffer A containing 6 M urea, 1 h each in 3, 1.5, and 0.75 M urea in buffer A and 0.05% Tween 20 and 1 h in buffer A with 0.05% Tween 20. The kinase assay is carried out for 1 h at 30?°C in the presence of 50 μM ATP, 5 μCi/ml [32P]ATP, 20 mM Hepes, pH 7.6, 20 mM MgCl2, 20 mM β-glycerophosphate, 20 mM p-nitrophenyl phosphate, 1 mM sodium vanadate, 2 mM dithiothreitol. The gel is washed with 5% trichloroacetic acid and 1% sodium pyrophosphate, dried, and exposed to film. A separate gel with no HIS-IκB-α is assayed as a control. |
| 體外活性 | 在含Caov-3細胞的無胸腺裸鼠體內(nèi),BAY 11-7085可使紫杉醇對腹內(nèi)傳播和腹水產(chǎn)生的抑制作用增強.BAY11-7085對腦膜炎相關(guān)的NF-κB活性增加有抑制作用,改善被感染大鼠臨床狀態(tài),并使腦膜炎相關(guān)的CNS并發(fā)癥和腦膜炎癥顯著衰減. |
| 體內(nèi)活性 | BAY 11-7085與紫杉醇聯(lián)用可增強對NF-κB活性的抑制,并使經(jīng)紫杉醇處理細胞的存活率降低。通過抑制NF-κB,BAY11-7085可抑制TNFα誘導(dǎo)的粘附分子E-selectin,ICAM-1及VCAM-1的表達。BAY11-7085（10 μM）對HUVEC細胞無細胞毒性。此外,Bay11-7085與LY294002聯(lián)用可協(xié)同影響PEL細胞的凋亡。 |
| 存儲條件 | 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 : 24.9 mg/mL (99.87 mM), Sonication is recommended.
Ethanol : 24.9 mg/mL (99.87 mM), Sonication is recommended.
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| 關(guān)鍵字 | Nuclear factor-κB | Nuclear factor-kappaB | NF-κB | NFκB | NF-kB | NFkB | IκBα?phosphorylation | IκB | Inhibitor | inhibit | IKK | IkB/IKK | IkB | Ferroptosis | BAY 11-7085 | Bay 11-7085 | Bay 117085 | Bay 11 7085 | Apoptosis |
| 相關(guān)產(chǎn)品 | L-Cystine | L-Glutamic acid | Cysteamine hydrochloride | Alginic acid | Stavudine | Dextran sulfate sodium salt (MW 4500-5500) | Tributyrin | L-Glutamine | L-Ascorbic acid sodium salt | L-Ascorbic acid | Sodium 4-phenylbutyrate | N,N-Dimethylacetamide |
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