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  1. Stem Cell/Wnt PI3K/Akt/mTOR Cell Cycle/DNA Damage Autophagy Anti-infection
  2. Organoid PI3K Polo-like Kinase (PLK) Autophagy Antibiotic
  3. Wortmannin

Wortmannin  (Synonyms: 渥曼青霉素; SL-2052; KY-12420)

目錄號(hào): HY-10197 純度: 99.85%
COA 產(chǎn)品使用指南

Wortmannin (SL-2052) 是一種有效的,不可逆的,選擇性PI3K 抑制劑,IC50 值為 3 nM。Wortmannin (SL-2052) 阻斷自噬 (autophagy) 形成,并有效抑制 Polo-like kinase 1 (PlK1)Plk3,IC50 值分別為 5.8 和 48 nM。

MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報(bào),我們不為任何個(gè)人用途提供產(chǎn)品和服務(wù)

Wortmannin Chemical Structure

Wortmannin Chemical Structure

CAS No. : 19545-26-7

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10 mM * 1 mL in DMSO ¥990
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1 mg ¥342
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5 mg ¥900
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10 mg ¥1500
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Customer Review

Other Forms of Wortmannin:

MCE 顧客使用本產(chǎn)品發(fā)表的 118 篇科研文獻(xiàn)

WB
Cell Viability Assay

    Wortmannin purchased from MCE. Usage Cited in: Cancer Cell Int. 2023 Apr 16;23(1):68.  [Abstract]

    Wortmannin (1 mM; 24 h) significantly reverses the PCK1-OE-induced increased expression of LC3B II in RKO and SW480 cells.

    Wortmannin purchased from MCE. Usage Cited in: Biopolymers. 2023 Mar 28.

    Wortmannin (2 μM; 2, 4, 6 h) decreases the expression of p-AKT and the ratio of p-AKT/AKT while increases the expression of p-ERK and the ratio of p-ERK/ERK in T84 cells.

    Wortmannin purchased from MCE. Usage Cited in: Biopolymers. 2023 Mar 28.

    Wortmannin (5.0, 10 μM; 24 h) significantly induces cell death in T84 cells.

    Wortmannin purchased from MCE. Usage Cited in: bioRxiv. 2023 Feb 14.

    Both of LY294002 (LY; 30 μM) and Wortmannin (Wort; 50 nM) can downregulate the expression of ACE2 in HPAEpiC cells.

    Wortmannin purchased from MCE. Usage Cited in: Cell Mol Life Sci. 2018 Jul;75(14):2627-2641.  [Abstract]

    RAW264.7 macrophages are pre-treated with the inhibitor of ERK, JNK, P38, P65, and AKT signal pathway.Western blot analyzes the non- and phosphorylation of ERK, JNK, P38, P65, and AKT.

    Wortmannin purchased from MCE. Usage Cited in: Arthritis Res Ther. 2018 Feb 7;20(1):20.  [Abstract]

    Cells preincubated with or without the NF-κB inhibitor PDTC (100 μM), the PI3K inhibitor Wortmannin (3 μg/mL), or DMSO-Control for 2 h. Total protein expression of ABCG2, PDZK1, Akt, p-Akt, and NF-κB p65 determined by western blot analysis. Protein expression normalized to that of GAPDH.
    • 生物活性

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    生物活性

    Wortmannin (SL-2052; KY-12420) is a potent, selective and irreversible PI3K inhibitor with an IC50 of 3 nM. Wortmannin also blocks autophagy formation, and potently inhibits Polo-like kinase 1 (PlK1) and Plk3 with IC50s of 5.8 and 48 nM, respectively[1][2][3].

    IC50 & Target[1][2][3]

    PI3K

    3 nM (IC50)

    DNA-PK

    16 nM (IC50)

    PLK3

    48 nM (IC50)

    ATM

    150 nM (IC50)

    ATR

    1.8 μM (IC50)

    MLCK

    200 nM (IC50)

    Autophagy

     

    細(xì)胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    A549 IC50
    0.22 μM
    Compound: wortmannin
    Inhibition of Plk3 in human A549 cells assessed as casein substrate phosphorylation by Western blot
    Inhibition of Plk3 in human A549 cells assessed as casein substrate phosphorylation by Western blot
    [PMID: 17135248]
    A549 IC50
    11.4 μM
    Compound: 1, wortmannin, Wm
    Antiproliferative activity against human A549 cells after 48 hrs by SRB method
    Antiproliferative activity against human A549 cells after 48 hrs by SRB method
    [PMID: 18630894]
    A549 IC50
    4.28 ng/mL
    Compound: wortmannin
    Cytotoxicity against human A549 cells after 24 hrs by YO-PRO-1 assay
    Cytotoxicity against human A549 cells after 24 hrs by YO-PRO-1 assay
    [PMID: 19138858]
    A549 IC50
    4.28 ng/mL
    Compound: wortmannin
    Cytotoxicity against human A549 cells after 24 hrs by propidium iodide assay
    Cytotoxicity against human A549 cells after 24 hrs by propidium iodide assay
    [PMID: 19138858]
    HeLa IC50
    49 nM
    Compound: wortmannin
    Inhibition of AX-7503 binding to recombinant Plk3 expressed in HeLa cells by Western blot
    Inhibition of AX-7503 binding to recombinant Plk3 expressed in HeLa cells by Western blot
    [PMID: 17135248]
    MCF7 IC50
    > 100 μM
    Compound: Wortmannin
    Cytotoxicity against human MCF7 cells after 72 hrs by MTS/PMS assay
    Cytotoxicity against human MCF7 cells after 72 hrs by MTS/PMS assay
    [PMID: 23040731]
    Sf9 IC50
    0.012 μM
    Compound: (+)-2
    Inhibition of human PI3Kalpha expressed in Sf9 cells by fluorescent polarization assay
    Inhibition of human PI3Kalpha expressed in Sf9 cells by fluorescent polarization assay
    [PMID: 21121631]
    體外研究
    (In Vitro)

    Wortmannin(0-100 nM;24-72 小時(shí))以時(shí)間和劑量依賴性方式抑制 K562 細(xì)胞增殖。24 小時(shí)、48 小時(shí)和 72 小時(shí)的 IC50 值分別為 25±0.10 nM、12.5±0.08 nM 和 6.25±0.11 nM[4]。 Wortmannin 可阻止 YAP 進(jìn)入核[6]。

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

    Cell Proliferation Assay[4]

    Cell Line: K562 cells
    Concentration: 0, 6.25, 12.5, 25, 50 and 100 nM
    Incubation Time: 0, 24, 48 and 72 hours
    Result: Inhibited the K562 cells proliferation. The IC50 value at 24 hour, 48 hour, and 72 hour was 25±0.10 nM, 12.5±0.08 nM, and 6.25±0.11 nM.
    體內(nèi)研究
    (In Vivo)

    Wortmannin(口服管飼法;每日;在 Scid 小鼠中;一組八只小鼠在全部 14 天內(nèi)均以 1 mg/kg 的劑量服用 Wortmannin。第二組八只小鼠在前 5 天以 1.5 mg/kg 的劑量服用 Wortmannin,其余治療期間劑量減少至 1 mg/kg)治療顯著減緩了小鼠 C3H 乳腺腫瘤和人類 MCF-7 乳腺癌異種移植瘤的生長(zhǎng)速度。與對(duì)照組相比,7 天 1 mg/kg Wortmannin 可使已患小鼠 C3H 乳腺腫瘤的小鼠的腫瘤負(fù)擔(dān)減少 54%。從腫瘤植入后 1 天開始,連續(xù) 14 天服用 1 mg/kg Wortmannin 后,人類 MCF-7 乳腺癌異種移植瘤負(fù)擔(dān)與對(duì)照組相比減少了 97%[5]。

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

    Animal Model: Scid mice with the murine C3H mammary tumor or human MCF-7 breast cancer xenograft[5]
    Dosage: 1 mg/kg and 1.5 mg/kg
    Administration: Oral gavage; daily; one group 1 mg/kg for 14 days; second group 1.5 mg/kg for 5 days then 1.0 mg/kg for 9 days.
    Result: The growth rate of the treated tumors was significantly slower during drug administration than that of nontreated tumors.
    分子量

    428.43

    Formula

    C23H24O8

    CAS 號(hào)
    性狀

    固體

    顏色

    White to yellow

    中文名稱

    渥曼青霉素;沃氏籃酶素;奧特曼寧

    初始來源
    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 : ≥ 50 mg/mL (116.71 mM; 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)

    * "≥" means soluble, but saturation unknown.

    配制儲(chǔ)備液
    濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
    1 mM 2.3341 mL 11.6705 mL 23.3410 mL
    5 mM 0.4668 mL 2.3341 mL 4.6682 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: 2.08 mg/mL (4.85 mM); 懸濁液; 超聲助溶

      此方案可獲得 2.08 mg/mL的均勻懸濁液,懸濁液可用于口服和腹腔注射。

      1 mL 工作液為例,取 100 μL 20.8 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% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.08 mg/mL (4.85 mM); 澄清溶液

      此方案可獲得 ≥ 2.08 mg/mL(飽和度未知)的澄清溶液。

      1 mL 工作液為例,取 100 μL 20.8 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中,混合均勻。

      2 g SBE-β-CD(磺丁基醚 β-環(huán)糊精)粉末定容于 10 mL 的生理鹽水中,完全溶解至澄清透明。
    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(gòu)。 ,Tween 80,均可在 MCE 網(wǎng)站選購(gòu)。
    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(guó)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: 99.86%

    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 2.3341 mL 11.6705 mL 23.3410 mL 58.3526 mL
    5 mM 0.4668 mL 2.3341 mL 4.6682 mL 11.6705 mL
    10 mM 0.2334 mL 1.1671 mL 2.3341 mL 5.8353 mL
    15 mM 0.1556 mL 0.7780 mL 1.5561 mL 3.8902 mL
    20 mM 0.1167 mL 0.5835 mL 1.1671 mL 2.9176 mL
    25 mM 0.0934 mL 0.4668 mL 0.9336 mL 2.3341 mL
    30 mM 0.0778 mL 0.3890 mL 0.7780 mL 1.9451 mL
    40 mM 0.0584 mL 0.2918 mL 0.5835 mL 1.4588 mL
    50 mM 0.0467 mL 0.2334 mL 0.4668 mL 1.1671 mL
    60 mM 0.0389 mL 0.1945 mL 0.3890 mL 0.9725 mL
    80 mM 0.0292 mL 0.1459 mL 0.2918 mL 0.7294 mL
    100 mM 0.0233 mL 0.1167 mL 0.2334 mL 0.5835 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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    產(chǎn)品名稱:
    Wortmannin
    目錄號(hào):
    HY-10197
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