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  1. JAK/STAT Signaling Stem Cell/Wnt
  2. STAT
  3. SH-4-54

SH-4-54是 STAT 的抑制劑,與 STAT3STAT5 結(jié)合的 KDs 值分別為300,464 nM。

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SH-4-54 Chemical Structure

SH-4-54 Chemical Structure

CAS No. : 1456632-40-8

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ¥1679
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1 mg ¥568
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5 mg ¥1250
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10 mg ¥2000
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25 mg ¥3600
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50 mg ¥5405
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100 mg 現(xiàn)貨 詢價(jià)
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500 mg   詢價(jià)  

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Customer Review

    SH-4-54 purchased from MCE. Usage Cited in: CNS Neurosci Ther. 2023 Mar 13.  [Abstract]

    SH-4-54 effectively blocks OGD/R-induced STAT3 phosphorylation in microglia.

    SH-4-54 purchased from MCE. Usage Cited in: Biochem Biophys Res Commun. 2017 Mar 4;484(2):311-317.  [Abstract]

    SGC7901 cells are pretreated with IL-6 neutralizing antibody or SH-4-54 for an hour prior to Tipα stimulation. STAT3 (Y705) phosphorylation is significantly inhibited by IL-6 antibody or SH-4-54 pretreatment.

    查看 STAT 亞型特異性產(chǎn)品:

    • 生物活性

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    生物活性

    SH-4-54 is a STAT inhibitor that binds to STAT3 and STAT5 with KDs of 300, 464 nM, respectively.

    IC50 & Target

    STAT3

    300 nM (Kd)

    STAT5

    464 nM (Kd)

    細(xì)胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    AGS IC50
    5.42 μM
    Compound: 4; SH4-54
    Antiproliferative activity against human AGS cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
    Antiproliferative activity against human AGS cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
    [PMID: 36170649]
    H9c2 IC50
    10.2 μM
    Compound: 4; SH4-54
    Antiproliferative activity against human H9c2 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
    Antiproliferative activity against human H9c2 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
    [PMID: 36170649]
    MGC-803 IC50
    8.51 μM
    Compound: 4; SH4-54
    Antiproliferative activity against human MGC-803 cells assessed as reduction in cell viability measured after 72 hrs by CCK-8 assay
    Antiproliferative activity against human MGC-803 cells assessed as reduction in cell viability measured after 72 hrs by CCK-8 assay
    [PMID: 36170649]
    體外研究
    (In Vitro)

    SH-4-54 potently kills glioblastoma brain cancer stem cells (BTSCs) and effectively suppresses STAT3 phosphorylation and its downstream transcriptional targets at low nM concentrations.SH-4-54 shows unprecedented cytotoxicity in human BTSCs, displays no toxicity in human fetal astrocytes, potently suppresses pSTAT3 with nanomolar IC50s, inhibiting STAT3's downstream targets, and shows no discernible off-target effects at therapeutic doses[1].

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

    體內(nèi)研究
    (In Vivo)

    SH-4-54 exhibits blood-brain barrier permeability potently controls glioma tumor growth, and inhibits pSTAT3 in vivo. SH-4-54 demonstrates the power of STAT3 inhibitors for the treatment of BTSCs and validates the therapeutic efficacy of a STAT3 inhibitor for GBM clinical application.SH-4-54 decreases pSTAT3 expression in tumor cells of treated mice. SH-4-54 appears to decrease proliferation and increase apoptosis of treated tumors[1].

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

    分子量

    610.59

    Formula

    C29H27F5N2O5S

    CAS 號(hào)
    性狀

    固體

    顏色

    White to off-white

    運(yùn)輸條件

    Room temperature in continental US; may vary elsewhere.

    儲(chǔ)存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    溶解性數(shù)據(jù)
    細(xì)胞實(shí)驗(yàn): 

    DMSO 中的溶解度 : 100 mg/mL (163.78 mM; 超聲助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響,請(qǐng)使用新開封的 DMSO)

    配制儲(chǔ)備液
    濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
    1 mM 1.6378 mL 8.1888 mL 16.3776 mL
    5 mM 0.3276 mL 1.6378 mL 3.2755 mL
    查看完整儲(chǔ)備液配制表

    * 請(qǐng)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(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
    儲(chǔ)備液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?年內(nèi)使用, -20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?年內(nèi)使用。

    • 摩爾計(jì)算器

    • 稀釋計(jì)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(dòng)物實(shí)驗(yàn):

    請(qǐng)根據(jù)您的 實(shí)驗(yàn)動(dòng)物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

    以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液,再依次添加助溶劑:
    ——為保證實(shí)驗(yàn)結(jié)果的可靠性,澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件,適當(dāng)保存;體內(nèi)實(shí)驗(yàn)的工作液,建議您現(xiàn)用現(xiàn)配,當(dāng)天使用;
    以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比;如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過加熱和/或超聲的方式助溶

    • 方案 一

      請(qǐng)依序添加每種溶劑: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (4.09 mM); 澄清溶液

      此方案可獲得 ≥ 2.5 mg/mL(飽和度未知)的澄清溶液。

      1 mL 工作液為例,取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 400 μL PEG300 中,混合均勻;再向上述體系中加入 50 μL Tween-80,混合均勻;然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

      生理鹽水的配制:將 0.9 g 氯化鈉,溶解于 ddH?O 并定容至 100 mL,可以得到澄清透明的生理鹽水溶液。
    • 方案 二

      請(qǐng)依序添加每種溶劑: 10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (4.09 mM); 澄清溶液

      此方案可獲得 ≥ 2.5 mg/mL(飽和度未知)的澄清溶液,此方案實(shí)驗(yàn)周期在半個(gè)月以上的動(dòng)物實(shí)驗(yàn)酌情使用。

      1 mL 工作液為例,取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL玉米油中,混合均勻。

    動(dòng)物溶解方案計(jì)算器
    請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息:

    給藥劑量

    mg/kg

    動(dòng)物的平均體重

    g

    每只動(dòng)物的給藥體積

    μL

    動(dòng)物數(shù)量

    由于實(shí)驗(yàn)過程有損耗,建議您多配一只動(dòng)物的量
    請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    如果您的動(dòng)物是免疫缺陷鼠或者體弱鼠,建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
    方案所需 助溶劑 包括:DMSO, ,均可在 MCE 網(wǎng)站選購。 ,Tween 80,均可在 MCE 網(wǎng)站選購。
    計(jì)算結(jié)果
    工作液所需濃度 : mg/mL
    儲(chǔ)備液配制方法 : mg 藥物溶于 μL  DMSO(母液濃度為 mg/mL)。
    您所需的儲(chǔ)備液濃度超過該產(chǎn)品的實(shí)測(cè)溶解度,以下方案僅供參考,如有需要,請(qǐng)與 MCE 中國技術(shù)支持聯(lián)系。
    動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)備液,加入 μL 。 μL ,混合均勻至澄清,再加 μL Tween 80,混合均勻至澄清,再加 μL 生理鹽水。
    連續(xù)給藥周期超過半月以上,請(qǐng)謹(jǐn)慎選擇該方案。
    請(qǐng)確保第一步儲(chǔ)備液溶解至澄清狀態(tài),從左到右依次添加助溶劑。您可采用超聲加熱 (超聲清洗儀,建議頻次 20-40 kHz),渦旋吹打等方式輔助溶解。
    純度 & 產(chǎn)品資料

    純度: 99.45%

    參考文獻(xiàn)

    完整儲(chǔ)備液配制表

    * 請(qǐng)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(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
    儲(chǔ)備液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?年內(nèi)使用, -20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?年內(nèi)使用。

    可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.6378 mL 8.1888 mL 16.3776 mL 40.9440 mL
    5 mM 0.3276 mL 1.6378 mL 3.2755 mL 8.1888 mL
    10 mM 0.1638 mL 0.8189 mL 1.6378 mL 4.0944 mL
    15 mM 0.1092 mL 0.5459 mL 1.0918 mL 2.7296 mL
    20 mM 0.0819 mL 0.4094 mL 0.8189 mL 2.0472 mL
    25 mM 0.0655 mL 0.3276 mL 0.6551 mL 1.6378 mL
    30 mM 0.0546 mL 0.2730 mL 0.5459 mL 1.3648 mL
    40 mM 0.0409 mL 0.2047 mL 0.4094 mL 1.0236 mL
    50 mM 0.0328 mL 0.1638 mL 0.3276 mL 0.8189 mL
    60 mM 0.0273 mL 0.1365 mL 0.2730 mL 0.6824 mL
    80 mM 0.0205 mL 0.1024 mL 0.2047 mL 0.5118 mL
    100 mM 0.0164 mL 0.0819 mL 0.1638 mL 0.4094 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:
    SH-4-54
    目錄號(hào):
    HY-16975
    需求量: