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

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

Cat. No.: HY-10197 Purity: 99.86%
COA Handling Instructions

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
Solution
10 mM * 1 mL in DMSO USD 99 In-stock
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10 mM * 1 mL
ready for reconstitution
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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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Customer Review

Based on 97 publication(s) in Google Scholar

Top Publications Citing Use of Products

91 Publications Citing Use of MCE Wortmannin

Cell Viability Assay
WB

    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.
    • Biological Activity

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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].

    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.
    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].

    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

    Appearance

    Solid

    Formula

    C23H24O8

    CAS No.
    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

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    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.
    In Vivo:
    • 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 available by MCE.
    Purity & Documentation

    Purity: 99.86%

    References
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    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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    Product Name:
    Wortmannin
    Cat. No.:
    HY-10197
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