AS1517499

For research use only.

Catalog No.S8685

9 publications

AS1517499 Chemical Structure

CAS No. 919486-40-1

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

Selleck's AS1517499 has been cited by 9 publications

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Biological Activity

Description AS1517499 is a novel and potent STAT6 inhibitor with an IC50 value of 21 nM.
Targets
STAT6 [1]
(Cell-free assay)
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].

Assay
Methods Test Index PMID
Western blot
p-STAT6 / STAT6 ; 

PubMed: 31363052     


BMMΦs were pretreated with STAT6 inhibitor AS1517499 (1 μM) for 1 h, followed by TSG6 (400 ng/mL; Left) or IL-4 (100 ng/mL; Right) stimulation for the indicated time points. Cell lysates were used for immunoblot analysis to determine STAT6 phosphorylation at Y641 and total STAT6 expression. Representative blots from three independent experiments are shown. *P < 0.05 vs. control.

31363052
Immunofluorescence
MUC5AC; 

PubMed: 28931396     


BECs were pretreated with specific STAT6 inhibitor (AS1517499) or a selective IκB kinase inhibitor (IKK 16) for half an hour, then treated for 24 h in the presence or absence of 20 ng/ml IL-4. Immunofluorescence staining of MUC5AC protein was performed.

28931396
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].

Protocol

Cell Research:

[2]

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  • Cell lines: Normal human BSM cells
  • Concentrations: 100 nM
  • Incubation Time: 30 min
  • Method:

    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.


    (Only for Reference)
Animal Research:

[2]

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  • Animal Models: A murine model of allergic bronchial asthma (Male BALB/c mice)
  • Dosages: 1 or 10 mg/kg/d
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 79 mg/mL (198.56 mM)
Ethanol 36 mg/mL (90.48 mM)
Water 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.

Chemical Information

Molecular Weight 397.86
Formula

C20H20ClN5O2

CAS No. 919486-40-1
Storage powder
in solvent
Synonyms N/A
Smiles C1=CC=C(C=C1)CNC2=NC(=NC=C2C(=O)N)NCCC3=CC(=C(C=C3)O)Cl

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID