1. PI3K/Akt/mTOR
    Autophagy
    Apoptosis
  2. Akt
    Autophagy
    Apoptosis
  3. Deguelin

Deguelin (Synonyms: (-)-Deguelin; (-)-cis-Deguelin)

Cat. No.: HY-13425 Purity: 99.29%
Handling Instructions

Deguelin, a naturally occurring rotenoid, acts as a chemopreventive agent by blocking multiple pathways like PI3K-Akt, IKK-NF-κB, and MAPK-mTOR-survivin-mediated apoptosis. Deguelin binding to Hsp90 leads to a decreased expression of numerous oncogenic proteins, including MEK1/2, Akt, HIF1α, COX-2, and NF-κB.

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

Deguelin Chemical Structure

Deguelin Chemical Structure

CAS No. : 522-17-8

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Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 59 In-stock
Estimated Time of Arrival: December 31
5 mg USD 54 In-stock
Estimated Time of Arrival: December 31
10 mg USD 100 In-stock
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50 mg USD 350 In-stock
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Customer Review

Based on 5 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Deguelin purchased from MCE. Usage Cited in: Int J Mol Med. 2018 Jun;41(6):3157-3166.

    MGC-803 and MKN-45 cells are treated with increasing doses of Deguelin (0, 1 and 10 μM) for 6 h and harvested for western blot (WB) analysis to assess the p-Akt signaling.

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    • Biological Activity

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    Description

    Deguelin, a naturally occurring rotenoid, acts as a chemopreventive agent by blocking multiple pathways like PI3K-Akt, IKK-NF-κB, and MAPK-mTOR-survivin-mediated apoptosis. Deguelin binding to Hsp90 leads to a decreased expression of numerous oncogenic proteins, including MEK1/2, Akt, HIF1α, COX-2, and NF-κB.

    IC50 & Target[2]

    Akt

     

    In Vitro

    Deguelin (0-500 nM) in a dose and time dependent manner inhibits the growth of MDA-MB-231, MDA-MB-468, BT-549 and BT-20 cells. Deguelin at all concentrations fails to reduce cell numbers in the presence of 1 ng EGF but in the presence of EGF 20 ng reinstated deguelin mediated growth inhibition. Deguelin treated cells show reduced expression of Survivin as determined by western blot and immunofluorescence examinations. Deguelin inhibits p-ERK and its downstream target p-STAT-3 and c-Myc expression in a dose dependent manner[1]. Deguelin down-regulates Akt signaling probably by disrupting its association with Hsp 90 in cultured HNSCC cells. Deguelin deguelin disrupts the association between Hsp 90 with survivin and Cdk4. Deguelin deguelin treatment increases cellular ceramide level through de novo synthase pathway to mediate HNSCC cell death and apoptosis[2]. Deguelin inhibits the proliferation of MPC-11 cells in a concentration- and time-dependent manner and causes the apoptotic death of MPC-11 cells. Following exposure to deguelin, the phosphorylation of Akt is decreased. Deguelin-induced apoptosis is characterized by the upregulation of Bax, downregulation of Bcl-2 and activation of caspase-3[3].

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

    In Vivo

    Deguelin (2 or 4 mg/kg, i.p.) reduces the in vivo tumor growth of MDA-MB-231 cells transplanted subcutaneously in athymic mice[1]. Deguelin (4 mg/kg, p.o.) treatment shows a great inhibition in tumor growth, which is demonstrated by reduced tumor size and improved mice survival and, indicating a significant anti-tumor ability by deguelin in vivo[2]. In the colon cancer xenograft model, the volume of the tumor treated with deguelin is significantly lower than that of the control, and the apoptotic index for deguelin-treated mice is much higher[4].

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

    Molecular Weight

    394.42

    Formula

    C₂₃H₂₂O₆

    CAS No.

    522-17-8

    SMILES

    O=C1[[email protected]]2([H])[[email protected]](COC3=CC(OC)=C(OC)C=C32)([H])OC4=C5C=CC(C)(C)OC5=CC=C14

    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 (126.77 mM; Need ultrasonic)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.5354 mL 12.6768 mL 25.3537 mL
    5 mM 0.5071 mL 2.5354 mL 5.0707 mL
    10 mM 0.2535 mL 1.2677 mL 2.5354 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: ≥ 2.5 mg/mL (6.34 mM); Clear solution

    • 2.

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

      Solubility: 2.5 mg/mL (6.34 mM); Suspended solution; Need ultrasonic

    • 3.

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

      Solubility: ≥ 2.5 mg/mL (6.34 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
    Kinase Assay
    [2]

    Caspase 3 activity is determined using Caspase-Glo-3 assays. This assay provides luminogenic substrate in a buffer system optimized for each specific caspase activity. The caspase cleavage of the substrate is followed by generation of a luminescent signal. The signal generated is proportional to the amount of caspase activity present in the sample. Protein (10 µg) from the cell samples is diluted in water to a final volume of 50 µL and added to a white 96-well microtitre plate, followed by 50 µL of Caspase-Glo-3 reagent. The plate is sealed and gently mixed at 300-500 rpm for 30 s and incubated at room temperature for 30 min. Luminescence is measured in a microplate reader (TECAN Infinite 200).

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

    Cell Assay
    [1]

    Breast cancer cells are incubated with increasing concentration of Deguelin ranging from 31 nM to 500 nM for 24, 48 and 72 h. At the termination the cells are trypsinized and cell proliferation is evaluated by counting cells using Z-series Coulter counter. Data are presented as Mean±SE percent of control.

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

    Animal Administration
    [1]

    Six to seven weeks old female athymic mice (nu/nu) are housed in a barrier free environment under 24±2°C temperature, 50±10% relative humidity, and 12-hour light/12-hour dark cycle. Mice are provided with sterile mouse chow and water ad libitum. MDA-MB-231 cells (3.0 million cells/animal) are suspended in sterile PBS and then injected subcutaneously into the dorsal flank region using 23 g hypodermic needle. Animals are observed daily for the growth of palpable tumor at the site of injection. Once the tumor (approximately 50 mm3) appears, the mice are randomized in to three groups, animals receiving either 1) vehicle as a control 2) Deguelin treatment at 2 mg/kg bodyweight dose or 3) Deguelin at 4 mg/kg body weight. Each group consists of 10 animals. Vehicle or Deguelin is administered through i.p. injection daily for 21 days. Animals are monitored daily for the signs of drug/vehicle associated toxicity and weighed once weekly. Growth of tumor at the site of cell injection is monitored every alternate day and of tumor size is measured using calipers. Tumor volume is calculated by using the well-established formula: tumor volume (mm3)=π/6 length×width×depth. Data represent the mean tumor volume+SE (mm3) in each group. The animals are sacrificed at the indicated time unless they appear to be moribund or tumors show sign of necrosis. At termination, the tumor is excised, freed from connective tissue and other organs, a small piece is fixed in 10% buffered formalin and remaining tumor is snap frozen for future biochemical analysis. Liver, lung, kidney and spleen are excised and weighed.

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

    References

    Purity: 99.29%

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    Keywords:

    Deguelin(-)-Deguelin (-)-cis-DeguelinAktAutophagyApoptosisPKBProtein kinase BInhibitorinhibitorinhibit

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