1. JAK/STAT Signaling
    Stem Cell/Wnt
  2. STAT

AS1517499 

Cat. No.: HY-100614 Purity: 99.17%
Handling Instructions

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

For research use only. We do not sell to patients.

AS1517499 Chemical Structure

AS1517499 Chemical Structure

CAS No. : 919486-40-1

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 110 In-stock
Estimated Time of Arrival: December 31
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10 mg USD 150 In-stock
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25 mg USD 300 In-stock
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50 mg USD 490 In-stock
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100 mg USD 750 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Top Publications Citing Use of Products

    AS1517499 purchased from MCE. Usage Cited in: Respir Res. 2017 Sep 20;18(1):174.

    BECs are 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 is performed according to the Methods.

    AS1517499 purchased from MCE. Usage Cited in: J Exp Med. 2018 Aug 6;215(8):2175-2195.

    Representative images of PCNA (green) and SMA (red) immunostaining of PASMCs cultured with DK-PGD2-treated Th2 cell medium with or without STAT6 inhibitor AS1517499.

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    • Biological Activity

    • Protocol

    • Technical Information

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    • References

    Description

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

    IC50 & Target

    IC50: 21 nM (STAT6)[1]

    In Vitro

    AS1517499 shows potent STAT6 inhibition with an IC50 value of 21 nM, and also inhibits IL-4-induced Th2 differentiation of mouse spleen T cells with an IC50 value of 2.3 nM and without influencing T-helper cell 1 (Th1) differentiation induced by IL-12. AS1517499 selectively inhibits Th2 differentiation without affecting Th1 differentiation[1]. In cultured human BSM cells, IL-13 (100 ng/mL) causes a phosphorylation of STAT6 and an up-regulation of RhoA, a monomeric GTPase responsible for Ca2+ sensitization of smooth muscle contraction: both events are inhibited by co-incubation with AS1517499 (100 nM)[2].

    In Vivo

    In BALB/c mice that are actively sensitized and repeatedly challenged with ovalbumin antigen, an increased IL-13 level in bronchoalveolar lavage fluids and a phosphorylation of STAT6 in bronchial tissues are observed after the last antigen challenge. These mice have an augmented BSM contractility to acetylcholine together with an up-regulation of RhoA in bronchial tissues. Intraperitoneal injections of AS1517499 (10 mg/kg) 1 hour before each ovalbumin exposure inhibits both the antigen-induced up-regulation of RhoA and BSM hyperresponsiveness, almost completely[2].

    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 35 mg/mL (87.97 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.5134 mL 12.5672 mL 25.1345 mL
    5 mM 0.5027 mL 2.5134 mL 5.0269 mL
    10 mM 0.2513 mL 1.2567 mL 2.5134 mL
    *Please refer to the solubility information to select the appropriate solvent.
    References
    Cell Assay
    [2]

    Normal human BSM cells (hBSMCs) are maintained in SmBM medium supplemented with 5% fetal bovine serum, 0.5 ng/mL human epidermal growth factor (hEGF), 5 μg/mL insulin, 2 ng/mL human fibroblast growth factor-basic (hFGF-b), 50 μg/mL gentamicin, and 50 ng/mL amphotericin B. Cells are maintained at 37°C 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 observed, cells are cultured without serum for 24 hours before addition of recombin is ant human IL-13. AS1517499 (100 nM) 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 (1 μM) 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[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [2]

    Mice[2]
    Male BALB/c mice are used. Preparation of a murine model of allergic bronchial asthma, which has an in vivo AHR, is performed. In brief, BALB/c mice (8 wk of age) are actively sensitized by intraperitoneal injections of 8 μg ovalbumin (OVA) with 2 mg Imject Alum on Day 0 and Day 5. The sensitized mice are challenged with aerosolized OVA-saline solution (5 mg/mL) for 30 minutes on Days 12, 16, and 20. A control group of mice received the same immunization procedure but inhaled saline aerosol instead of OVA challenge. The aerosol is generated with an ultrasonic nebulizer and introduced to a Plexiglas chamber box (130×200 mm, 100 mm height) in which the mice are placed. Animals also received intraperitoneal injection with AS1517499 (1 or 10 mg/kg/d; dissolved in 20% DMSO in saline) or its vehicle 1 hour before each antigen inhalation (Days 12, 16, and 20). Twenty-four hours after the last OVA challenge, mice are killed by exsanguination from abdominal aorta under urethane (1.6 g/kg, intraperitoneally) anesthesia.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    397.86

    Formula

    C₂₀H₂₀ClN₅O₂

    CAS No.

    919486-40-1

    SMILES

    O=C(C1=CN=C(NCCC2=CC=C(O)C(Cl)=C2)N=C1NCC3=CC=CC=C3)N

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

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    Product Name:
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    Cat. No.:
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    Cat. No.: HY-100614