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

WP1066 是一种新颖的 JAK2 和 STAT3 抑制剂，对 STAT5 和 ERK1/2 也起作用，但对 JAK1 和 JAK3 没有影响。

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WP1066 Chemical Structure

WP1066 Chemical Structure

CAS No. : 857064-38-1

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3.  试用装只面向终端客户。

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥506
In-stock
5 mg ￥460
In-stock
10 mg ￥810
In-stock
50 mg ￥3095
In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

Customer Review

WP1066 相关抗体

Top Publications Citing Use of Products

    WP1066 purchased from MCE. 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 MCE. 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 MCE. 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 MCE. 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.

    查看 STAT 亚型特异性产品:

    查看所有亚型
    STAT3 STAT5 STAT6 STAT1

    查看 JAK 亚型特异性产品:

    查看所有亚型
    JAK1 JAK2 JAK3 Tyk2 JAK

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    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

     

    细胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    HeLa IC50
    4.2 μM
    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 μM
    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 μM
    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 μM
    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]
    体外研究
    (In Vitro)

    WP1066 以剂量依赖的方式显著抑制 HEL 细胞的生长。抑制 HEL 细胞增殖的 IC50 值为 2.3 μM。WP1066 抑制携带 JAK2 V617F 突变亚型的人 HEL 细胞的生长[1]。用 WP1066 阻断 p-STAT3，增强了 CTX 对肿瘤的细胞毒性作用。WP1066 对 B16 细胞的 IC50 剂量为 2.43 μM (0.865 μg/mL)[2]。WP1066 抑制 AML 母细胞集落形成细胞增殖，在浓度升高时抑制正常 BM 祖细胞增殖，并抑制 AML 集落形成细胞增殖[3]。

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

    WP1066 相关抗体:
    体内研究
    (In Vivo)

    WP1066 (30 mg/kg，og) 对肿瘤微环境中 p-STAT3 通路的 CTX 抑制作用产生累加效应[2]。

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Clinical Trial
    分子量

    356.22

    Formula

    C17H14BrN3O
    CAS 号
    性状

    固体

    颜色

    Off-white to light yellow

    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    溶解性数据
    细胞实验： 

    DMSO 中的溶解度 : ≥ 44 mg/mL (123.52 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

    Ethanol 中的溶解度 : 16.67 mg/mL (46.80 mM; 超声助溶)

    * "≥" means soluble, but saturation unknown.

    配制储备液
    浓度 溶剂体积 质量 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
    查看完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
    储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

    • 摩尔计算器

    • 稀释计算器

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

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    动物溶解方案计算器
    请输入动物实验的基本信息：

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    只
    由于实验过程有损耗，建议您多配一只动物的量
    计算结果
    工作液所需浓度 : mg/mL
    纯度 & 产品资料

    纯度: 99.77%

    COA (193 KB) LCMS (95 KB)

    产品使用指南 (1538 KB)
    参考文献
    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.
    参考文献

    WP1066 相关分类

    完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
    储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

    可选溶剂 浓度 溶剂体积 质量 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
    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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    目录号：
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