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受注：045-509-1970 |
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化学情報
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Synonyms | RWJ 64809, PB 203580 | Storage (From the date of receipt) |
3 years-20°C （in the dark）powder |
| 化学式 | C21H16FN3OS |
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| 分子量 | 377.43 | CAS No. | 152121-47-6 | |
| Solubility (25°C)* | 体外 | DMSO | 96 mg/mL warmed with 50ºC water bath (254.35 mM) | |
| Ethanol | 28 mg/mL (74.18 mM) | |||
| Water | Insoluble | |||
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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 | Adezmapimod (SB203580, RWJ 64809, PB 203580) is a p38 MAPK inhibitor with IC50 of 0.3-0.5 μM in THP-1 cells, 10-fold less sensitive to SAPK3(106T) and SAPK4(106T) and blocks PKB phosphorylation with IC50 of 3-5 μM. SB203580 induces mitophagy and autophagy. |
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| in vitro | SB203580 inhibits the IL-2-induced proliferation of primary human T cells, murine CT6 T cells, or BAF F7 B cells with an IC50 of 3–5 μm. SB203580 also inhibits IL-2-induced p70S6 kinase activation, although the concentration required is slightly higher with an IC50 above 10 μm. SB203580 also inhibits the activity of PDK1 in a dose-dependent manner with an IC50 in the 3–10 μm range. [1] SB203580 inhibits p38-MAPK stimulation of MAPKAPK2 with an IC50 of approximately 0.07 μM, whereas inhibits total SAPK/JNK activity with an IC50 of 3–10 μM. SB203580 at higher concentrations activates the ERK pathway, which subsequently enhances NF-κB transcriptional activity. [2] SB203580 induces autophagy in human hepatocellular carcinoma (HCC) cells. [3] |
| in vivo | SB203580 protects pig myocardium against ischemic injury in an in vivo model. [4]SB203580 is effective to prevent and treat the disease in MRL/lpr mice model of Systemic lupus erythematosus (SLE). [5] |
| 特徴 | First reported p38 inhibitor. |
プロトコル(参考用のみ)
| キナーゼアッセイ | Cellular receptor kinase phosphorylation assay | |
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| 4 μg of sheep anti-PKBα is immobilized on 25 μL of protein G-Sepharose overnight (or 1.5 hours) and washed in Buffer A (50 mm Tris, pH 7.5, 1 mm EDTA, 1 mm EGTA, 0.5 mm Na3VO4, 0.1% β-mercaptoethanol, 1% Triton X-100, 50 mm sodium fluoride, 5 mm sodium pyrophosphate, 0.1 mm phenylmethylsulfonyl fluoride, 1 μg/mL aprotinin, pepstatin, leupeptin, and 1 μm microcystin). The immobilized anti-PKB is then incubated with 0.5 ml of lysate (from 5 × 106 cells) for 1.5 hours and washed three times in 0.5 mL of Buffer A supplemented with 0.5 m NaCl, two times in 0.5 mL of Buffer B (50 mm Tris-HCl, pH 7.5, 0.03% (w/v) Brij-35, 0.1 mm EGTA, and 0.1% β-mercaptoethanol), and twice with 100 μl of assay dilution buffer; 5× assay dilution buffer is 100 mm MOPS, pH 7.2, 125 mm β-glycerophosphate, 25 mm EGTA, 5 mm sodium orthovanadate, 5 mm DTT. To the PKB enzyme immune complex is added 10 μL of assay dilution buffer, 40 μm protein kinase A inhibitor peptide, 100 μm PKB-specific substrate peptide, and 10 μCi of [γ-32P]ATP, all made up in assay dilution buffer. The reaction is incubated for 20 minutes at room temperature with shaking, then samples are pulse spun, and 40 μL of reaction volume are removed into another tube to which is added 20 μL of 40% trichloroacetic acid to stop the reaction. This is mixed and incubated for 5 minutes at room temperature, and 40 μL is transferred onto P81 phosphocellulose paper and allowed to bind for 30 seconds. The P81 piece is washed three times in 0.75% phosphoric acid then in acetone at room temperature. γ-32P incorporation is then measured by scintillation counting. | ||
| 細胞アッセイ | 細胞株 | CT6 cell , BA/F3 F7 cell |
| 濃度 | 0–30 μM | |
| 反応時間 | 1 hour | |
| 実験の流れ | CT6 cell and BA/F3 F7 cell are rested by washing three times in RPMI and culturing overnight in RPMI, 5% fetal calf serum in the absence of growth factor, antibiotics, or β-mercaptoethanol supplements. 2–5 × 106 rested CT6 cells are resuspended in 2 mL of RPMI, 5% fetal calf serum and preincubated with SB203580 or vehicle control as indicated in figure legends. Cells are then stimulated with 20 ng/ml recombinant human IL-2 for 5 minutes at 37 °C and pelleted in a minifuge for 30 seconds, medium is aspirated, and the pellet is lysed in the appropriate buffer. BA/F3 cells stably expressing deletion mutants of IL-2 receptor β chain are maintained in glutamine containing RPMI further supplemented with 5% fetal calf serum and 0.2 μg/mL G418. The cells are then washed extensively, rested overnight, and washed again before activating with IL-2; such cell preparations are >90% T cells. Cellular proliferation assays are performed by measurement of [3H]thymidine incorporation. |
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| 動物実験 | 動物モデル | Systemic lupus erythematosus (SLE) are established in female MRL/lpr mice and female C57BL/6 mice |
| 投薬量 | 0.1 M/day | |
| 投与方法 | Orally administered | |
参考
カスタマーフィードバック
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Data from [J Biol Chem, 2010, 285, 32824-32833]
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Data from [J Biol Chem, 2010, 285, 32824–32833]
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Data from [J Biol Chem, 2010, 285, 32824–32833]
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| Bactericidal/permeability-increasing protein instructs dendritic cells to elicit Th22 cell response [ Cell Rep, 2024, 43(3):113929] | PubMed: 38457343 |
| Ammonia stress-induced heat shock factor 1 enhances white spot syndrome virus infection by targeting the interferon-like system in shrimp [ mBio, 2024, e0313623.] | PubMed: 38358252 |
| Securinine inhibits the tumor growth of human bladder cancer cells by suppressing Wnt/β-catenin signaling pathway and activating p38 and JNK signaling pathways [ Biochem Pharmacol, 2024, 223:116125] | PubMed: 38484850 |
| ERK1/2-CEBPB Axis-Regulated hBD1 Enhances Anti-Tuberculosis Capacity in Alveolar Type II Epithelial Cells [ Int J Mol Sci, 2024, 25(4)2408] | PubMed: 38397085 |
| PCSK9 increases vulnerability of carotid plaque by promoting mitochondrial dysfunction and apoptosis of vascular smooth muscle cells [ CNS Neurosci Ther, 2024, 30(2):e14640] | PubMed: 38402551 |
| FGF18 alleviates sepsis-induced acute lung injury by inhibiting the NF-κB pathway [ Respir Res, 2024, 25(1):108] | PubMed: 38419044 |
| Licochalcone A induces mitochondria-dependent apoptosis and interacts with venetoclax in acute myeloid leukemia [ Eur J Pharmacol, 2024, 968:176418] | PubMed: 38350590 |
| Antioxidant and Antimelanogenic Activities of Lactobacillus kunkeei NCHBL-003 Isolated from Honeybees [ Microorganisms, 2024, 12(1)188] | PubMed: 38258014 |
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。