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

WP1066 

Cat. No.: HY-15312 Purity: 99.67%
Data Sheet SDS Handling Instructions

WP1066 is a novel inhibitor of JAK2 and STAT3, and also shows effect on STAT5 and ERK1/2, without affecting JAK1 and JAK3.

For research use only. We do not sell to patients.
WP1066 Chemical Structure

WP1066 Chemical Structure

CAS No. : 857064-38-1

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $77 In-stock
10 mg $70 In-stock
50 mg $210 In-stock
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

    WP1066 purchased from MCE. Usage Cited in: Free Radic Biol Med. 2017 Apr 17;108:542-553.

    The role of STAT3 in SERPINB1-mediated protecting ALI in OALT is further confirmed by using STAT3 specific inhibitor WP1066. post-OALT lung STAT3 activation is significantly increased evidenced by elevated phosphorylation of STAT3 at site727 and site705 (P<0.01 vs sham), which are associated with enhanced HO-1 protein expression.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    WP1066 is a novel inhibitor of JAK2 and STAT3, and also shows effect on STAT5 and ERK1/2, without affecting JAK1 and JAK3.

    IC50 & Target

    IC50: 2.3 μM (JAK2), 2.43 μM (STAT3)

    In Vitro

    WP1066 markedly inhibits the growth of HEL cells in a dose-dependent manner. The IC50 value for inhibition of the proliferation of HEL cells is 2.3 μM. WP1066 inhibits the growth of human HEL cells carrying the JAK2 V617F mutant isoform[1]. Blockade of p-STAT3 with WP1066 enhances the cytotoxic effects of CTX on the tumor. The IC50 doses of WP1066 for B16 cells is 2.43 µM (0.865 µg/mL)[2]. WP1066 inhibits AML blast colony-forming cell proliferation, suppresses normal BM progenitor proliferation at increased concentrations, and inhibits AML colony-forming cell proliferation[3].

    In Vivo

    WP1066 (30 mg/kg, o.g.)does not further enhance the therapeutic effects of cyclophosphamide on pulmonary melanoma lesions, enhance the therapeutic effects of cyclophosphamide against CNS melanoma, or further enhance immune-mediated cytotoxic effects of CTX in C57BL/6J mice. WP1066 exerts an additive effect to CTX inhibition of the p-STAT3 pathway within the tumor microenvironment[2].

    Clinical Trial
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    References
    Preparing Stock Solutions
    Concentration Volume Mass 1 mg 5 mg 10 mg
    1 mM 2.8073 mL 14.0363 mL 28.0725 mL
    5 mM 0.5615 mL 2.8073 mL 5.6145 mL
    10 mM 0.2807 mL 1.4036 mL 2.8073 mL
    Please refer to the solubility information to select the appropriate solvent.
    Cell Assay
    [1]

    WP1066 is dissolved in 1% DMSO, diluted with a 5% dextrose solution.

    Briefly, fresh low-density peripheral blood cells and various cell lines at the logarithmic phase of their growth are washed twice in RPMI 1640 containing 10% FCS and counted in a hemocytometer. Cell viability is assessed by the trypan blue (0.1%) staining method. Equal numbers of viable cells (5×104 per well) are incubated in a total volume of 100 μL of RPMI 1640 supplemented with 10% FCS alone or with WP1066 at increasing concentrations; the incubations are continued for up to 72 h in 96-well flat-bottomed plates at 37°C in a humidified 5% CO2 atmosphere. Experiments for each condition are done in triplicate. After incubation, 20 μL of CellTiter96 One Solution Reagent are added to each well. The plates are then incubated for an additional 60 min at 37°C in a humidified 5% CO2 atmosphere. Immediately after incubation, absorbance is read using a 96-well plate reader at a wavelength of 490 nm. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [2]

    WP1066 is formulated in vehicle of DMSO:polyethylene glycol (PEG) 300 (1:4 ratio).

    To ascertain the inhibition of the immune populations within the spleen and peripheral blood compartments, tumor-bearing mice are treated with CTX, WP1066, or CTX in combination with WP1066, for 14 days. Single-cell suspensions are prepared from spleens and the peripheral blood of mice and single cells are surface-stained with FITC-conjugated anti-CD4 (L3T4) or PE-conjugated anti-CD8 (53-6.7) and are intracellularly stained with APC-conjugated-FoxP3 (clone FJK-16s). The cell number of CD4+ and CD8+ T cells in the peripheral blood is counted based on positive surface staining of the respective markers relative to the total cell count of PBMCs. The percentage of FoxP3+ Tregs is calculated within the peripheral blood and within the CD4 compartment. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    356.22

    Formula

    C₁₇H₁₄BrN₃O

    CAS No.

    857064-38-1

    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

    Solvent & Solubility

    DMSO: ≥ 44 mg/mL

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    Purity: 99.67%

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    Inquiry Information

    Product Name:
    WP1066
    Cat. No.:
    HY-15312
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