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受注：045-509-1970 |
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化学情報
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Synonyms | Nsc75890 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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| 化学式 | C14H8N2O |
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| 分子量 | 220.23 | CAS No. | 129-56-6 | ||||
| Solubility (25°C)* | 体外 | DMSO | 44 mg/mL (199.79 mM) | ||||
| Water | Insoluble | ||||||
| Ethanol | Insoluble | ||||||
| 体内 （毎回新しく調製した物を用意してください） |
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* <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. |
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溶剤液（一定の濃度）を調合する
生物活性
| 製品説明 | SP600125（Nsc75890）は、JNK1、JNK2、JNK3に対する広範なJNK阻害剤であり、細胞フリーアッセイでのIC50はそれぞれ40nM、40nM、90nMです。MKK4に対して10倍、MKK3、MKK6、PKB、PKCαに対して25倍、ERK2、p38、Chk1、EGFRなどに対して100倍高い選択性を示します。SP600125は、Aurora kinase A、FLT3、TRKAを含むserine/threonine kinasesの広範な阻害剤でもあり、IC50はそれぞれ60nM、90nM、70nMです。SP600125はautophagyを阻害し、apoptosisを活性化します。 |
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| in vitro | SP600125 is originally characterized as a selective ATP-competitive inhibitor of c-Jun N-terminal kinase JNK. In Jurkat T cells, this compound inhibits the phosphorylation of c-Jun with IC50 of 5 μM to 10 μM. In CD4+ cells, such as Th0 cells isolated from either human cord or peripheral blood, it blocks cell activation and differentiation and inhibits the expression of inflammatory genes COX-2, IL-2, IL-10, IFN-γ, and TNF-α, with IC50 of 5 μM to 12 μM. However, later studies reveal that this chemical also suppresses aryl hydrocarbon receptor (AhR) , Mps1 , and a panel of other serine/threonine kinases, including Aurora kinase A, FLT3, MELK, and TRKA . In a mouse beta cells MIN6, this compound (20 μM) induces the phosphorylation of p38 MAPK and its downstream CREB-dependent promoter activation. In HCT116 cells, it (20 μM) blocks the G2 phase to mitosis transition and induces endoreplication. This ability of this inhibitor is independent of JNK inhibition, but due to its inhibition of CDK1-cyclin B activation upstream of Aurora A and Polo-like kinase 1. |
| in vivo | In mice, SP600600125 (15 mg/kg or 30 mg/kg) significantly inhibits lipopolysaccharide (LPS)-induced TNF-α expression and anti-CD3-induced apoptosis of CD4+ CD8+ thymocytes. |
プロトコル(参考用のみ)
| キナーゼアッセイ | In Vitro Kinase Assays | |
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| The potency of SP600125 towards kinases, including MPS1, JNK, and Aurora kinase A, is determined based on the specific measurement of radioactive phosphotransfer to the substrate. For each enzyme, the absolute Km values for ATP and the specific substrate are initially determined and each assay is then run at optimized [ATP] (2·αKm) and [substrate] (5·Km) concentrations. MPS1 activity is measured using 5 nM of MPS1 recombinant protein in 50 mM HEPES pH 7.5, 2.5 mM MgCl2, 1 mM MnCl2, 1 mM DTT, 3 μM NaVO3, 2 mM β-glycerophosphate, 0.2 mg/mL BSA, 200 μM P38-βtide substrate-peptide (KRQADEEMTGYVATRWYRAE), and 8 μM ATP with 1.5 nM 33P-γ-ATP. Ten serial 1:3 dilutions (from 30 μM to 1.5 nM) of this compound are tested and IC50 determined. | ||
| 細胞アッセイ | 細胞株 | HCT116, A2780, and U2OS cells |
| 濃度 | 0–5 μM | |
| 反応時間 | 72 hours | |
| 実験の流れ | Cells are seeded in 384 well-plates. One day after seeding, the cells are treated with SP600125 for 72 hours and the plates are then processed using a CellTiter-Glo assay. Inhibitory activity is evaluated comparing treated versus control data and IC50 value of proliferation is calculated. |
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| 動物実験 | 動物モデル | Mouse LPS/TNF model (female CD-1) |
| 投薬量 | 15 or 30 mg/kg | |
| 投与方法 | Administered via intravenous injection or orally | |
参考
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カスタマーフィードバック
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Data from [Cancer Res, 2013, 73(20):6346-58]
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Data from [Biochim Biophys Acta, 2012, 1823(5), 987-96]
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, , Lee lay hoon from National University of Singapore
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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。