AS1517499

SKU: orb1302826

Description

AS1517499 is a potent small molecule inhibitor of STAT6 phosphorylation with an IC50 of 21 nM. It is capable of crossing the blood-brain barrier, making it a valuable research tool for investigating STAT6-mediated pathways in both cellular assays and in vivo models of neuroinflammation and immune disorders.

Research Area

Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 919486-40-1
• MW: 397.86
• Purity: 99.30% (May vary between batches)
• Formula: C₂₀H₂₀ClN₅O₂
• SMILES: NC(=O)c1cnc(NCCc2ccc(O)c(Cl)c2)nc1NCc1ccccc1
• Target: STAT
• Solubility: DMSO:262.5 mg/mL (659.78 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (12.57 mM)

Bioactivity

• Target IC50:
  STAT6 (HBSM cells):21 nM|RhoA (HBSM cells):21 nM|STAT6:21 nM
• In Vivo:
  METHODS: To investigate the effect of AS1517499 on the development of antigen-induced BSM hyperreactivity, AS1517499 (10 mg/kg) was administered intraperitoneally to mice 1 hour before each ovalbumin exposure. RESULTS: AS1517499 completely inhibited the antigenicity induced upregulation of RhoA and BSM hyperreactivity.
• In Vitro:
  METHODS: Western Blot was used to detect the expression levels of AS1517499 in human BSM cells treated with 100 nM AS1517499. RESULTS: Treatment of BSM cells with AS1517499 inhibited IL-13-induced STAT6 phosphorylation and up-regulation of RhoA.
• Cell Research:
  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 (hFGFb), 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 .
• Animal Research:
  Mice

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

AS 1517499, AS1517499, AS-1517499, inhibit, Inhibitor, STAT, STAT6

Compound Identifiers

PubChem CID

10340781