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

WP1066 是一種新穎的 JAK2STAT3 抑制劑,對 STAT5 和 ERK1/2 也起作用,但對 JAK1JAK3 沒有影響。

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WP1066 Chemical Structure

WP1066 Chemical Structure

CAS No. : 857064-38-1

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     可免費(fèi)申領(lǐng)三個不同產(chǎn)品的試用裝。

3.  試用裝只面向終端客戶。

規(guī)格 價格 是否有貨 數(shù)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   詢價  
200 mg   詢價  

* Please select Quantity before adding items.

Customer Review

    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 亞型特異性產(chǎn)品:

    查看 JAK 亞型特異性產(chǎn)品:

    • 生物活性

    • 實驗參考方法

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    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

     

    體外研究
    (In Vitro)

    WP1066 以劑量依賴的方式顯著抑制 HEL 細(xì)胞的生長。抑制 HEL 細(xì)胞增殖的 IC50 值為 2.3 μM。WP1066 抑制攜帶 JAK2 V617F 突變亞型的人 HEL 細(xì)胞的生長[1]。用 WP1066 阻斷 p-STAT3,增強(qiáng)了 CTX 對腫瘤的細(xì)胞毒性作用。WP1066 對 B16 細(xì)胞的 IC50 劑量為 2.43 μM (0.865 μg/mL)[2]。WP1066 抑制 AML 母細(xì)胞集落形成細(xì)胞增殖,在濃度升高時抑制正常 BM 祖細(xì)胞增殖,并抑制 AML 集落形成細(xì)胞增殖[3]。

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

    體內(nèi)研究
    (In Vivo)

    WP1066 (30 mg/kg,og) 對腫瘤微環(huán)境中 p-STAT3 通路的 CTX 抑制作用產(chǎn)生累加效應(yīng)[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 號
    性狀

    固體

    顏色

    Off-white to light yellow

    運(yùn)輸條件

    Room temperature in continental US; may vary elsewhere.

    儲存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    溶解性數(shù)據(jù)
    細(xì)胞實驗: 

    DMSO 中的溶解度 : ≥ 44 mg/mL (123.52 mM; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響,請使用新開封的 DMSO)

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

    * "≥" means soluble, but saturation unknown.

    配制儲備液
    濃度 溶劑體積 質(zhì)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
    查看完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C儲存時,請在6個月內(nèi)使用,-20°C儲存時,請在1個月內(nèi)使用。

    • 摩爾計算器

    • 稀釋計算器

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

    質(zhì)量
    =
    濃度
    ×
    體積
    ×
    分子量 *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    濃度 (start)

    C1

    ×
    體積 (start)

    V1

    =
    濃度 (final)

    C2

    ×
    體積 (final)

    V2

    動物溶解方案計算器
    請輸入動物實驗的基本信息:

    給藥劑量

    mg/kg

    動物的平均體重

    g

    每只動物的給藥體積

    μL

    動物數(shù)量

    由于實驗過程有損耗,建議您多配一只動物的量
    計算結(jié)果
    工作液所需濃度 : mg/mL
    純度 & 產(chǎn)品資料

    純度: 99.77%

    參考文獻(xiàn)
    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.

    參考文獻(xiàn)

    完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效
    儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C儲存時,請在6個月內(nèi)使用,-20°C儲存時,請在1個月內(nèi)使用。

    可選溶劑 濃度 溶劑體積 質(zhì)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.

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    Inquiry Information

    產(chǎn)品名稱:
    WP1066
    目錄號:
    HY-15312
    需求量: