1. PI3K/Akt/mTOR
    Cell Cycle/DNA Damage
    Autophagy
  2. PI3K
    Polo-like Kinase (PLK)
    Autophagy
  3. Wortmannin

Wortmannin (Synonyms: SL-2052; KY-12420)

製品番号: HY-10197 純度: 99.85%
取扱説明書

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

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Wortmannin 構造式

Wortmannin 構造式

CAS 番号 : 19545-26-7

容量 価格(税別) 在庫状況 数量
10 mM * 1 mL in DMSO USD 88 在庫あり
Estimated Time of Arrival: December 31
5 mg USD 80 在庫あり
Estimated Time of Arrival: December 31
10 mg USD 110 在庫あり
Estimated Time of Arrival: December 31
25 mg USD 220 在庫あり
Estimated Time of Arrival: December 31
50 mg   お問い合わせ  
100 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

カスタマーレビュー

Based on 13 publication(s) in Google Scholar

Top Publications Citing Use of Products

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

    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.

    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.

    PI3K アイソフォーム固有の製品をすべて表示:

    Polo-like Kinase (PLK) アイソフォーム固有の製品をすべて表示:

    • 生物活性

    • 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

    Wortmannin (SL-2052) is a potent, selective and irreversible PI3K inhibitor with an IC50 of 3 nM. wortmannin (SL-2052) 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

     

    体外実験

    Wortmannin (0-100 nM; 24-72 hours) inhibits the proliferation of K562 cells in a time- and dose-dependent manner. The IC50 values at 24 hour, 48 hour, and 72 hour are 25±0.10 nM, 12.5±0.08 nM, and 6.25±0.11 nM, respectively[4].

    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.
    体内実験

    Wortmannin (oral gavage; daily; in Scid mice; one group of eight mice is dosed with Wortmannin 1 mg/kg for all 14 days. The second group of eight mice is dosed with Wortmannin 1.5 mg/kg for the first 5 days and the dose is decreased to 1 mg/kg for the remaining treatment period) treatment significantly slower the growth rate of murine C3H mammary tumor and human MCF-7 breast cancer xenograft. A dose of 1 mg/kg Wortmannin for 7 days decrease the tumor burdens in mice with established murine C3H mammary tumors by 54% relative to controls. Human MCF-7 breast cancer xenograft burdens are decreased by 97% relative to controls after 14 days of 1 mg/kg Wortmannin beginning 1 day after tumor implantation[5].

    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

    分子式

    C₂₃H₂₄O₈

    CAS 番号

    19545-26-7

    SMILES

    O=C1C([[email protected]@](CC2)([H])[[email protected]@]3(C)C2=O)=C([[email protected]](OC(C)=O)C3)[[email protected]]4(C)C5=C1OC=C5C(O[[email protected]@H]4COC)=O

    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 : ≥ 50 mg/mL (116.71 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    10 mM 0.2334 mL 1.1671 mL 2.3341 mL
    *Please refer to the solubility information to select the appropriate solvent.
    体内:
    • 1.

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

      Solubility: 2.08 mg/mL (4.85 mM); Suspended solution; Need ultrasonic

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.08 mg/mL (4.85 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.08 mg/mL (4.85 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    参考文献

    純度: 99.85%

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    Keywords:

    WortmanninSL-2052KY-12420SL2052SL 2052KY12420KY 12420PI3KPolo-like Kinase (PLK)AutophagyPhosphoinositide 3-kinaseInhibitorinhibitorinhibit

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    製品名:
    Wortmannin
    製品番号:
    HY-10197
    数量:
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