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

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

Cat. No.: HY-10197 Purity: 99.85%
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Wortmannin (SL-2052; KY-12420) est un PI3K inhibiteur puissant, sélectif et irréversible avec un IC50 de 3 nM. Wortmannin bloque également la formation d'autophagie et inhibe puissamment la kinase de type Polo 1 (PlK1) et Plk3 avec IC50< sous> de 5,8 et 48 nM, respectivement.

Wortmannin (SL-2052; KY-12420) ist ein potenter, selektiver und irreversibler PI3K-Inhibitor mit einer IC50 von 3 nM. Wortmannin blockiert auch die Bildung von autophagy und hemmt potent die Polo-like kinase 1 (PlK1) und Plk3 mit einer IC50 von 5,8 bzw. 48 nM.
Wortmannin prevents nuclear entry of YAP.

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.

For research use only. We do not sell to patients.

Wortmannin Chemical Structure

Wortmannin Chemical Structure

CAS No. : 19545-26-7

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 99 In-stock
Solution
10 mM * 1 mL in DMSO USD 99 In-stock
Solid
1 mg USD 42 In-stock
5 mg USD 90 In-stock
10 mg USD 150 In-stock
50 mg USD 520 In-stock
100 mg USD 830 In-stock
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Based on 122 publication(s) in Google Scholar

Other Forms of Wortmannin:

Wortmannin Related Antibodies

Top Publications Citing Use of Products

116 Publications Citing Use of MCE Wortmannin

WB
Cell Viability Assay

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

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

    Wortmannin purchased from MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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.

    View All PI3K Isoform Specific Products:

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    PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

    View All Polo-like Kinase (PLK) Isoform Specific Products:

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    PLK1 PLK2 PLK3 PLK4

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    • Biological Activity

    • Purity & Documentation

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    Description

    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

     

    In Vitro

    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]. Wortmannin prevents nuclear entry of YAP[6].

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

    Wortmannin Related Antibodies

    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.
    In Vivo

    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].

    MedChemExpress (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.
    Molecular Weight

    428.43

    Formula

    C23H24O8
    CAS No.
    Appearance

    Solid

    Color

    White to yellow

    SMILES

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

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 50 mg/mL (116.71 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" 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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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    • Dilution Calculator

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

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

    V1

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    C2

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 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

      This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 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

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.86%

    COA (267 KB) LCMS (95 KB) Elemental Analysis Report (124 KB)

    Handling Instructions (2659 KB)
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 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
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    Wortmannin Related Classifications

    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:

    Wortmannin19545-26-7SL-2052 KY-12420SL2052SL 2052KY12420KY 12420KY-12420OrganoidPI3KPolo-like Kinase (PLK)AutophagyAntibioticPhosphoinositide 3-kinaseInhibitorinhibitorinhibit

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