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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 | C20H20ClN5O2 |
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分子量 | 397.86 | CAS No. | 919486-40-1 | |
Solubility (25°C)* | 体外 | DMSO | 80 mg/mL (201.07 mM) | |
Ethanol | 20 mg/mL (50.26 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 | AS1517499 is a novel and potent STAT6 inhibitor with an IC50 value of 21 nM. |
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in vitro | AS1517499 inhibit IL-4-induced Th2 differentiation of mouse spleen T cells, but has no influence on Th1 differentiation induced by IL-12[1]. AS1517499 is able to prevent the IL-4-activated STAT6-mediated increase of the clonogenic potential of primary PCa cells. At a dose of 300 nM, AS1517499 decreases the clonogenic potential of primary basal PCa cells[3]. |
in vivo | In vivo treatment with AS1517499 ameliorates the antigen-induced bronchial smooth muscle (BSM) hyperresponsiveness by inhibiting the RhoA up-regulation in BSMs and, at least in part, by reducing the IL-13 production in the airways in mice[2]. AS1517499 reduces preventive effects of apoptotic cell instillation on bleomycin-induced lung fibrosis by suppressing PPARγ[4]. |
細胞アッセイ | 細胞株 | Normal human BSM cells |
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濃度 | 100 nM | |
反応時間 | 30 min | |
実験の流れ | Cells are maintained in SmBM medium supplemented with 5% fetal bovine serum, 0.5 ng/ml human epidermal growth factor (hEGF), 5 mg/ml insulin, 2 ng/ml human fibroblast growth factor-basic (hFGF-b), 50 mg/ml gentamicin, and 50 ng/ml amphotericin B. Cells are maintained at 37℃ in a humidified atmosphere (5% CO2), fed every 48 to 72 hours, and passaged when cells reached 90 to 95% confluence. Then the hBSMCs (passages 7-9) are seeded in 6-well plates and 8-well chamber slides at a density of 3,500 cells/cm2 and, when 80 to 85% confluence is observed, cells are cultured without serum for 24 hours before addition of recombinant human IL-13. AS1517499, or its vehicle (0.3% DMSO) is treated 30 minutes before the addition of IL-13 (100 ng/ml). In some experiments, AS1517499 is treated 0 (co-incubation), 3, or 12 hours after the addition of IL-13. In another series of experiments, a selective Rho-kinase inhibitor Y-27632 or its vehicle (0.3% DMSO) is also applied 15 minutes before the IL-13 application. At the indicated time after the IL-13 treatment, cells are washed with PBS, immediately collected, and disrupted with 1×SDS sample buffer (250 μl/well), and used for Western blot analyses. |
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動物実験 | 動物モデル | A murine model of allergic bronchial asthma (Male BALB/c mice) |
投薬量 | 1 or 10 mg/kg/d | |
投与方法 | i.p. |
Transcriptional and chromatin profiling of human blood innate lymphoid cell subsets sheds light on HIV-1 pathogenesis [ EMBO J, 2023, e114153.] | PubMed: 37382276 |
JAK-STAT signalling shapes the NF-κB response in CLL towards venetoclax sensitivity or resistance via Bcl-XL [ Mol Oncol, 2023, 17(6):1112-1128] | PubMed: 36550750 |
Co-induced Allergic Response to an Unrelated Allergen Exacerbates Imiquimod-Induced Psoriasis in Mice [ Biol Pharm Bull, 2023, 46(10):1484-1489] | PubMed: 37599076 |
A novel targeted iron oxide nanocarrier for inhibiting M2-type macrophages in the tumor microenvironment [ Journal of Cancer Research and Therapeutics, 2022-, 18(5):p 1409-1416] | PubMed: None |
Ketone body β-hydroxybutyrate ameliorates colitis by promoting M2 macrophage polarization through the STAT6-dependent signaling pathway [ BMC Med, 2022, 20(1):148] | PubMed: 35422042 |
STAT6 contributes to renal fibrosis by modulating PPARα-mediated tubular fatty acid oxidation [ Cell Death Dis, 2022, 13(1):66] | PubMed: 35046382 |
Soluble SIRP-Alpha Promotes Murine Acute Lung Injury Through Suppressing Macrophage Phagocytosis [ Front Immunol, 2022, 13:865579] | PubMed: 35634325 |
Therapeutic Targeting of Cancer Stem Cells Prevents Resistance of Colorectal Cancer Cells to MEK Inhibition [ ACS Pharmacol Transl Sci, 2022, 5(9):724-734] | PubMed: 36110381 |
Dabigatran activates inflammation resolution by promoting fibrinogen-like protein 2 shedding and RvD5n-3 DPA production [ Theranostics, 2021, 11(9):4251-4261] | PubMed: 33754059 |
Tumor-derived microparticles promote the progression of triple-negative breast cancer via PD-L1-associated immune suppression [ Cancer Lett, 2021, 523:43-56] | PubMed: 34601021 |
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。