2. JAK/STAT Signaling Stem Cell/Wnt Protein Tyrosine Kinase/RTK Epigenetics Apoptosis
  3. STAT JAK Apoptosis
  4. WP1066

WP1066 is an 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
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 62 In-stock
Solution
10 mM * 1 mL in DMSO USD 62 In-stock
Solid
1 mg USD 29 In-stock
5 mg USD 57 In-stock
10 mg USD 92 In-stock
50 mg USD 277 In-stock
100 mg   Get quote  
200 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 28 publication(s) in Google Scholar

WP1066 Related Antibodies

Top Publications Citing Use of Products

    WP1066 purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2020 Feb;41(2):218-228.   [Abstract]

    HUVECs are pretreated with WP1066 for 1 h, followed by ZYZ-803 (1 μM) for 30 min. Protein levels are assessed by Western blot.

    WP1066 purchased from MedChemExpress. Usage Cited in: Cancer Manag Res. 2018 Nov 26;10:6339-6355.   [Abstract]

    Western blotting analysis: treatment with the Stat3 inhibitor WP1066 neutralizes the up-regulation of MMP2 and MMP9 and reverses the EMT progression caused by the overexpression of Uck2 in Bel-7402 cells.

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

    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.

    WP1066 purchased from MedChemExpress. Usage Cited in: J Cancer. 2017 Feb 25;8(5):816-824.  [Abstract]

    The protein expression levels of p-Akt, t-Akt, p-STAT3, t-STAT3, MMP2 and MMP9 are determined via western blotting 48 h after knockdown of B7-H3 and blockade of the PI3K/Akt pathway using LY294002 or the STAT3 pathway using WP1066.

    View All STAT Isoform Specific Products:

    View All Isoforms
    STAT3 STAT5 STAT6 STAT1

    View All JAK Isoform Specific Products:

    View All Isoforms
    JAK1 JAK2 JAK3 Tyk2 JAK

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

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

    IC50 & Target[1][2]

    JAK2

     

    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].

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

    WP1066 Related Antibodies
    In Vivo

    WP1066 (30 mg/kg, o.g.) exerts an additive effect to CTX inhibition of the p-STAT3 pathway within the tumor microenvironment[2].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    Clinical Trial
    Molecular Weight

    356.22

    Formula

    C17H14BrN3O
    CAS No.
    Appearance

    Solid

    Color

    Off-white to light yellow

    SMILES

    O=C(N[C@H](C1=CC=CC=C1)C)/C(C#N)=C/C2=NC(Br)=CC=C2
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 44 mg/mL (123.52 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Ethanol : 16.67 mg/mL (46.80 mM; Need ultrasonic)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent 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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

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    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

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    g

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    (per animal)

    μL

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    Purity & Documentation

    Purity: 99.77%

    COA (249 KB) LCMS (95 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [1]

    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]

    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

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    Ethanol / DMSO 1 mM 2.8073 mL 14.0363 mL 28.0725 mL 70.1813 mL
    5 mM 0.5615 mL 2.8073 mL 5.6145 mL 14.0363 mL
    10 mM 0.2807 mL 1.4036 mL 2.8073 mL 7.0181 mL
    15 mM 0.1872 mL 0.9358 mL 1.8715 mL 4.6788 mL
    20 mM 0.1404 mL 0.7018 mL 1.4036 mL 3.5091 mL
    25 mM 0.1123 mL 0.5615 mL 1.1229 mL 2.8073 mL
    30 mM 0.0936 mL 0.4679 mL 0.9358 mL 2.3394 mL
    40 mM 0.0702 mL 0.3509 mL 0.7018 mL 1.7545 mL
    DMSO 50 mM 0.0561 mL 0.2807 mL 0.5615 mL 1.4036 mL
    60 mM 0.0468 mL 0.2339 mL 0.4679 mL 1.1697 mL
    80 mM 0.0351 mL 0.1755 mL 0.3509 mL 0.8773 mL
    100 mM 0.0281 mL 0.1404 mL 0.2807 mL 0.7018 mL
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    WP1066 Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    WP1066857064-38-1WP 1066WP-1066STATJAKApoptosisJanus kinaseInhibitorinhibitorinhibit

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