AS1517499

製品コードS8685 バッチS868502

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C20H20ClN5O2
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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 AS1517499 is a novel and potent STAT6 inhibitor with an IC50 value of 21 nM.
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].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 Normal human BSM cells
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.
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.

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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。

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