受注:045-509-1970 |
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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C24H21N3OS |
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分子量 | 399.51 | CAS No. | 303162-79-0 | |
Solubility (25°C)* | 体外 | DMSO | 80 mg/mL (200.24 mM) | |
Ethanol | 16 mg/mL (40.04 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 | TAK-715 is a p38 MAPK inhibitor for p38α with IC50 of 7.1 nM, 28-fold more selective for p38α over p38β, no inhibition to p38γ/δ, JNK1, ERK1, IKKβ, MEKK1 or TAK1. Phase 2. |
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in vitro | TAK 715 inhibits LPS-stimulated release of TNF-alpha from THP-1 with IC50 of 48 nM. [1] TAK 715 (10 μM) inhibits Wnt-3a-induced hDvl2 phosphorylation and the hDvl2 shift in U2OS-EFC cells. [2] The amide NH of TAK 715 is hydrogen bonded to the main-chain carbonyl of Met109 of p38 alpha. TAK 715 binds relatively high in the ATP pocket, occupying the hydrophobic back pocket, the adenine region and the front pocket of p38 as well as extending to most of the length of the Gly-rich loop. [3] |
in vivo | TAK 715 (10 mg/kg, po) inhibits LPS-induced TNF-alpha production in mice with 87.6% inhibition. TAK 715 has a modest mouse bioavailability of 18.4% and a slightly improved rat bioavailability of 21.1%. TAK 715 has a modest mouse bioavailability of 18.4% and a slightly improved rat bioavailability of 21.1%. TAK 715 results in Cmax of 0.19 μg/mL and AUC(0-24 hours) of 1.16 μg·h/mL in rats. TAK 715 (30 mg/kg, po) significantly reduces the secondary paw volume with 25 % inhibition in a rat adjuvant-induced arthritis (AA) model. [1] |
キナーゼアッセイ | p38 MAP Kinase Assay | |
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Kinase reactions of purified human p38 MAP kinase α are performed at 30 °C for 1 h in kinase reaction buffer (25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol) containing 0.1 μCi [γ-32P]ATP, 500 nM ATP, and myelin basic protein (MBP). The kinase reactions are terminated by the addition of 10% trichloroacetic acid. Phosphorylated proteins are filtrated through GF/C filter plates with a Cell harvester, washing out free [γ-32P]ATP with 250 mM phosphoric acid. The plates are then incubated for 60 min at 45 °C, followed by the addition of 40 μL of MicroScint-O. Radioactivity is counted using a Top-count scintillation counter. | ||
動物実験 | 動物モデル | Adjuvant-induced arthritis (AA) rat model |
投薬量 | 30 mg/kg | |
投与方法 | Orally |
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Suppression of Lipid Accumulation in the Differentiation of 3T3-L1 Preadipocytes and Human Adipose Stem Cells into Adipocytes by TAK-715, a Specific Inhibitor of p38 MAPK [ Life (Basel), 2023, 13(2)412] | PubMed: 36836769 |
Oleanolic acid induces HCT116 colon cancer cell death through the p38/FOXO3a/Sirt6 pathway [ Chem Biol Interact, 2022, 363:110010] | PubMed: 35690101 |
Inhibition of endothelin-B receptor signaling synergizes with MAPK pathway inhibitors in BRAF mutated melanoma [ Oncogene, 2021, 10.1038/s41388-020-01628-x] | PubMed: 33500549 |
The Global Phosphorylation Landscape of SARS-CoV-2 Infection [ Cell, 2020, 182(3):685-712.e19] | PubMed: 32645325 |
The Global Phosphorylation Landscape of SARS-CoV-2 Infection [ Cell, 2020, 182(3):685-712.e19] | PubMed: 32645325 |
Mapping phospho-catalytic dependencies of therapy-resistant tumours reveals actionable vulnerabilities. [ Nat Cell Biol, 2019, 21(6):778-790] | PubMed: 31160710 |
Elucidating essential kinases of endothelin signalling by logic modelling of phosphoproteomics data [ Mol Syst Biol, 2019, 15(8):e8828] | PubMed: 31464372 |
Clinically Advanced p38 Inhibitors Suppress DUX4 Expression in Cellular and Animal Models of Facioscapulohumeral Muscular Dystrophy. [ J Pharmacol Exp Ther, 2019, 370(2):219-230] | PubMed: 31189728 |
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。