Home JAK/STAT STAT inhibitor AS1517499 For research use only.

AS1517499

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

AS1517499 Chemical Structure

AS1517499 Chemical Structure

CAS No. 919486-40-1

Purity & Quality Control

AS1517499 Related Products

Signaling Pathway

STAT Signaling Pathways

STAT Signaling Pathway

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
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].
Cell Research 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.
Experimental Result Images Methods Biomarkers Images PMID
Western blot p-STAT6 / STAT6 31363052
Immunofluorescence MUC5AC 28931396
In Vivo
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].
Animal Research Animal Models A murine model of allergic bronchial asthma (Male BALB/c mice)
Dosages 1 or 10 mg/kg/d
Administration i.p.

Chemical Information & Solubility

Molecular Weight 397.86 Formula

C20H20ClN5O2
CAS No. 919486-40-1 SDF --
Smiles C1=CC=C(C=C1)CNC2=NC(=NC=C2C(=O)N)NCCC3=CC(=C(C=C3)O)Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 79 mg/mL ( (198.56 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 36 mg/mL

Water : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

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.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy AS1517499 | AS1517499 supplier | purchase AS1517499 | AS1517499 cost | AS1517499 manufacturer | order AS1517499 | AS1517499 distributor