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は、IC50値が21 nMの新規強力なSTAT6阻害剤です。
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. This compound 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, this chemical decreases the clonogenic potential of primary basal PCa cells.
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. This compound reduces preventive effects of apoptotic cell instillation on bleomycin-induced lung fibrosis by suppressing PPARγ.

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, this compound 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.

参考

  • https://pubmed.ncbi.nlm.nih.gov/17071093/
  • https://pubmed.ncbi.nlm.nih.gov/19202006/
  • https://pubmed.ncbi.nlm.nih.gov/28553931/
  • https://pubmed.ncbi.nlm.nih.gov/29510393/

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：

Preadipocyte IL-13/IL-13Rα1 signaling regulates beige adipogenesis through modulation of PPARγ activity [ J Clin Invest, 2025, e169152] PubMed: 40198135
Heme oxygenase 1 confers gilteritinib resistance in FLT3-ITD acute myeloid leukemia in a STAT6-dependent manner [ Cancer Cell Int, 2025, 25(1):129] PubMed: 40186248
Targeting synergetic endothelial inflammation by inhibiting NFKB and JAK-STAT pathways [ iScience, 2025, 28(9):113307] PubMed: 40894883
Suberosin attenuates rheumatoid arthritis by repolarizing macrophages and inhibiting synovitis via the JAK/STAT signaling pathway [ Arthritis Res Ther, 2025, 27(1):12] PubMed: 39838477
Distinct Hodgkin lymphoma subtypes defined by noninvasive genomic profiling [ Nature, 2024, 625(7996):778-787] PubMed: 38081297
Targeted knockdown of PGAM5 in synovial macrophages efficiently alleviates osteoarthritis [ Bone Res, 2024, 12(1):15] PubMed: 38433252
Nicotinamide phosphoribosyltransferase prompts bleomycin-induced pulmonary fibrosis by driving macrophage M2 polarization in mice [ Theranostics, 2024, 14(7):2794-2815] PubMed: 38773984
Tonic type 2 immunity is a critical tissue checkpoint controlling autoimmunity in the skin [ Cell Rep, 2024, 43(7):114364] PubMed: 38900635
Guided monocyte fate to FRβ/CD163+ S1 macrophage antagonises atopic dermatitis via fibroblastic matrices in mouse hypodermis [ Cell Mol Life Sci, 2024, 82(1):14] PubMed: 39720957
Blocking M2-Like Macrophage Polarization Using Decoy Oligodeoxynucleotide-Based Gene Therapy Prevents Immune Evasion for Pancreatic Cancer Treatment [ Mol Cancer Ther, 2024, 23(10):1431-1445] PubMed: 38907533

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。