受注:045-509-1970 |
技術サポート:[email protected] 平日9:00〜18:00 1営業日以内にご連絡を差し上げます |
Synonyms | Bay 11-7083 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
|
化学式 | C13H15NO2S |
|||
分子量 | 249.33 | CAS No. | 196309-76-9 | |
Solubility (25°C)* | 体外 | DMSO | 50 mg/mL (200.53 mM) | |
Ethanol | 50 mg/mL (200.53 mM) | |||
Water | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
製品説明 | BAY 11-7085 (Bay 11-7083) is an irreversible inhibitor of TNFα-induced IκBα phosphorylation with IC50 of 10 μM. |
---|---|
in vitro | BAY 11-7085 inhibits TNFα-induced expression of adhesion molecules E-selectin, VCAM-1, and ICAM-1 by inhibition of NF-κB without detectable cytotoxicity at 10 μM in HUVEC cells. [1] BAY 11-7085 enhances the inhibition of NFkappaB activity by paclitaxel and decreases the viability of cells treated with paclitaxel. [3] Besides, combination of Bay11-7085 and LY294002 leads to synergistic apoptotic effect in PEL cells. [4] |
in vivo | BAY 11-7085 inhibits the meningitis-associated increase in NF-κB activity, and results in an improvement of the clinical status of infected rats and a marked attenuation of meningitis-associated CNS complications and meningeal inflammation. [2] BAY 11-7085 increases the efficacy of paclitaxel-induced inhibition of intraabdominal dissemination and production of ascites in athymic nude mice bearing Caov-3 cells. [3] |
特徴 | Selective IκBα phosphorylation inhibitor. |
キナーゼアッセイ | 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. | ||
細胞アッセイ | 細胞株 | HUVEC cells |
濃度 | ~20 μM | |
反応時間 | 16 hours | |
実験の流れ | Human umbilical vein endothelial cells (HUVEC) are isolated and maintained in culture. Cell toxicity is assessed by morphology and by MTT assay. | |
動物実験 | 動物モデル | Rat model of pneumococcal meningitis |
投薬量 | PBS | |
投与方法 | i.p. |
Data from [Data independently produced by , , Cell Physiol Biochem, 2015, 36(6):2466-79]
Data from [Data independently produced by , , Biochem Biophys Res Commun, 2018, 503(1):94-101]
Data from [Data independently produced by , , Leuk Res, 2017, 54:17-24]
SGK3 promotes vascular calcification via Pit-1 in chronic kidney disease [ Theranostics, 2024, 14(2):861-878] | PubMed: 38169564 |
Involvement of CCL2 in Salivary Gland Response to Hyperosmolar Stress Related to Sjögren's Syndrome [ Int J Mol Sci, 2024, 25(2)915] | PubMed: 38255988 |
Macrophages facilitate tumor cell PD-L1 expression via an IL-1β-centered loop to attenuate immune checkpoint blockade [ MedComm (2020), 2023, 4(2):e242] | PubMed: 37009412 |
Macrophages facilitate tumor cell PD-L1 expression via an IL-1β-centered loop to attenuate immune checkpoint blockade [ MedComm (2020), 2023, 4(2):e242] | PubMed: 37009412 |
The linear ANRIL transcript P14AS regulates the NF-κB signaling to promote colon cancer progression [ Mol Med, 2023, 29(1):162] | PubMed: 38041015 |
Integrative analysis of drug response and clinical outcome in acute myeloid leukemia [ Cancer Cell, 2022, S1535-6108(22)00312-9] | PubMed: 35868306 |
Proteogenomics refines the molecular classification of chronic lymphocytic leukemia [ Nat Commun, 2022, 13(1):6226] | PubMed: 36266272 |
Proteogenomics refines the molecular classification of chronic lymphocytic leukemia [ Nat Commun, 2022, 13(1):6226] | PubMed: 36266272 |
HOXA5-Mediated Stabilization of IκBα Inhibits the NF-κB Pathway and Suppresses Malignant Transformation of Breast Epithelial Cells [ Cancer Res, 2022, 82-20:3802-3814] | PubMed: 36166646 |
Drug-microenvironment perturbations reveal resistance mechanisms and prognostic subgroups in CLL [ Mol Syst Biol, 2022, 18(8):e10855] | PubMed: 35959629 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。