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. WP1066 can cross the blood-brain barrier[1][2][3][4].

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CAS 番号 : 857064-38-1

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>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 62 在庫あり
Solution
10 mM * 1 mL in DMSO USD 62 在庫あり
Solid
5 mg $57 在庫あり
10 mg $92 在庫あり
25 mg $180 在庫あり
50 mg $277 在庫あり
100 mg $378 在庫あり
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カスタマーレビュー

Based on 38 publication(s) in Google Scholar

WP1066 関連抗体

Top Publications Citing Use of Products

顧客検証

WB

    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 Jul: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.

    STAT アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    STAT3 STAT5 STAT6 STAT1

    JAK アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    JAK1 JAK2 JAK3 Tyk2 JAK

    • 生物活性

    • プロトコル

    • 純度とドキュメンテーション

    • 参考文献

    • カスタマーレビュー

    製品説明

    WP1066 is an inhibitor of JAK2 and STAT3, and also shows effect on STAT5 and ERK1/2, without affecting JAK1 and JAK3. WP1066 can cross the blood-brain barrier[1][2][3][4].

    IC50 & Target[1][2]

    JAK2

     

    STAT3

     

    Cellular Effect
    Cell Line Type Value Description References
    HeLa IC50
    4.2 3
    Compound: WP1066
    Cytotoxicity against human HeLa cells assessed as inhibition of cell viability measured after 48 hrs by MTT assay
    Cytotoxicity against human HeLa cells assessed as inhibition of cell viability measured after 48 hrs by MTT assay
    		[PMID: 34055214]
    HeLa IC50
    4.2 3
    Compound: WP1066
    Cytotoxicity against human HeLa cells assessed as inhibition of cell viability measured after 48 hrs by MTT assay
    Cytotoxicity against human HeLa cells assessed as inhibition of cell viability measured after 48 hrs by MTT assay
    		[PMID: 34055214]
    U-266 IC50
    1.5 3
    Compound: WP1066
    Antitumor activity against human U266 cells after 24 to 72 hrs by MTT assay
    Antitumor activity against human U266 cells after 24 to 72 hrs by MTT assay
    		[PMID: 22036213]
    U-266 IC50
    1.5 3
    Compound: WP1066
    Antitumor activity against human U266 cells after 24 to 72 hrs by MTT assay
    Antitumor activity against human U266 cells after 24 to 72 hrs by MTT assay
    		[PMID: 22036213]
    U-373MG ATCC IC50
    3.7 3
    Compound: WP1066
    Antitumor activity against human U373MG cells after 24 to 72 hrs by MTT assay
    Antitumor activity against human U373MG cells after 24 to 72 hrs by MTT assay
    		[PMID: 22036213]
    U-373MG ATCC IC50
    3.7 3
    Compound: WP1066
    Antitumor activity against human U373MG cells after 24 to 72 hrs by MTT assay
    Antitumor activity against human U373MG cells after 24 to 72 hrs by MTT assay
    		[PMID: 22036213]
    U-87MG ATCC IC50
    5.6 3
    Compound: WP1066
    Antitumor activity against human U87MG cells after 24 to 72 hrs by MTT assay
    Antitumor activity against human U87MG cells after 24 to 72 hrs by MTT assay
    		[PMID: 22036213]
    U-87MG ATCC IC50
    5.6 3
    Compound: WP1066
    Antitumor activity against human U87MG cells after 24 to 72 hrs by MTT assay
    Antitumor activity against human U87MG cells after 24 to 72 hrs by MTT assay
    		[PMID: 22036213]
    HeLa IC50
    4.2 3
    Compound: WP1066
    Cytotoxicity against human HeLa cells assessed as inhibition of cell viability measured after 48 hrs by MTT assay
    Cytotoxicity against human HeLa cells assessed as inhibition of cell viability measured after 48 hrs by MTT assay
    		[PMID: 34055214]
    U-266 IC50
    1.5 3
    Compound: WP1066
    Antitumor activity against human U266 cells after 24 to 72 hrs by MTT assay
    Antitumor activity against human U266 cells after 24 to 72 hrs by MTT assay
    		[PMID: 22036213]
    U-373MG ATCC IC50
    3.7 3
    Compound: WP1066
    Antitumor activity against human U373MG cells after 24 to 72 hrs by MTT assay
    Antitumor activity against human U373MG cells after 24 to 72 hrs by MTT assay
    		[PMID: 22036213]
    U-87MG ATCC IC50
    5.6 3
    Compound: WP1066
    Antitumor activity against human U87MG cells after 24 to 72 hrs by MTT assay
    Antitumor activity against human U87MG cells after 24 to 72 hrs by MTT assay
    		[PMID: 22036213]
    体外実験

    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 関連抗体
    体内実験

    WP1066 (30 mg/kg, o.g.) exerts an additive effect to CTX inhibition of the p-STAT3 pathway within the tumor microenvironment[2].
    WP1066 shows excellent CNS penetration provided compelling rationale for testing WP1066 against a variety cancer[4].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    臨床実験
    分子量

    356.22

    分子式

    C17H14BrN3O
    CAS 番号
    Appearance

    Solid

    Color

    White to light yellow

    SMILES

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

    Room temperature in continental US; may vary elsewhere.
    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    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
    10 mM 0.2807 mL 1.4036 mL 2.8073 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.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
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    ×
    Volume
    ×
    Molecular Weight *

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

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始）

    C1

    ×
    体積 （開始）

    V1

    =
    濃度 （終了）

    C2

    ×
    体積 （終了）

    V2

    体内:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 5 mg/mL (14.04 mM); Clear solution

      This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    純度とドキュメンテーション

    純度: 99.77%

    COA (249 KB) LCMS (95 KB)

    取扱説明書 (2659 KB)
    参考文献
    細胞実験
    [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.

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    動物実験
    [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.

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    参考文献

    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
    • No file chosen (Maximum size is: 1024 Kb)
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    • Your name will appear on the site.

    WP1066 Related Classifications

    • Molarity Calculator

    • Dilution Calculator

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    The dilution calculator equation

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

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
    × = ×
    C1   V1   C2   V2
    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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    製品番号:
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