Deguelin

Catalog No.S8132 Batch:S813201

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Technical Data

Formula

C23H22O6
Molecular Weight 394.42 CAS No. 522-17-8
Solubility (25°C)* In vitro DMSO 78 mg/mL (197.75 mM)
Ethanol 78 mg/mL (197.75 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description Deguelin, a natural product isolated from plants in the Mundulea sericea family, is an PI3K/AKT Inhibitor.
Targets
PI3K [1] Akt [1]
In vitro Deguelin downregulates Akt phosphorylation in leukaemia cell lines with an active PI3K/Akt axis. At 10 or 100 nmol/l, deguelin is effective in inhibiting Akt phosphorylation. Total Akt expression is unchanged by deguelin. Moreover, deguelin does not affect the expression or the phosphorylation levels of either p44/42 or p38 MAP kinases in U937 cells. Deguelin increases sensitivity of human leukaemia cells to chemotherapeutic drugs. Deguelin dephosphorylates Akt and increases cytarabine sensitivity of AML blasts but not of CB CD34+. Deguelin, when employed for 24 h at 10 nmol/l, causes an S phase arrest of U937 cells, with interference of progression to G2/M phase. While employed alone up to a concentration of 10 nmol/l for 24 h, Deguelin does not significantly increase the apoptotic rate of U937 cells[1].
In vivo Deguelin inhibits in vivo angiogenesis of chick chorioallantoic membrane (CAM) without cytotoxic effect and significantly reduces laser-induced CNV in a mouse model of AMD without significant retinal toxicity[2]. It exhibited significant anti-tumorigenesis and anti-proliferative activity in various types of cancer both in vitro and in vivo. In pre-clinical trials, deguelin markedly decreased the tumor incidence. Topically-administered deguelin significantly suppressed the multiplicity of skin tumors with UVB-induction, indicating its effect as a potential cancer chemopreventive agent. In A/J mice, deguelin clearly reduced the tumor multiplicity and volume, as well as the overall tumor burden with exposure to the tobacco-specific carcinogen benzo(a)pyrene (Bap) and other carcinogens, with no detectable toxicity. Nevertheless, the toxicity of deguelin over a certain dose should not be neglected. Treatment with deguelin, a potential mitochondria complex I inhibitor, reduced tyrosine hydroxylase-positive neurons, leading to Parkinson’s disease. Kim et al shows that deguelin promoted a PD-like syndrome, mainly by Src/STAT signaling, since α-synuclein (a key protein function in the pathogenesis of PD) was phosphorylated by deguelin-activated Src[3].

Protocol (from reference)

Cell Assay:[1]
  • Cell lines

    U937 cells

  • Concentrations

    1 nM, 10 nM, 100 nM

  • Incubation Time

    24 h

  • Method

    Flow cytometric analysis of cell cycle in response to deguelin. Cells are incubated with the indicated concentrations of deguelin for 24 h, then analysed for DNA content and for the percentage of cells in specific phases of the cell cycle by means of PI staining, whereas for detection of apoptotic cells the Annexin-FITC staining was employed. For this reason, the sum of apoptotic cells plus cells in various phases of the cell cycle exceeds 100%.

Animal Study:[4]
  • Animal Models

    A/J mice

  • Dosages

    5.0 or 10.0 mg/kg

  • Administration

    by gavage

Selleck's Deguelin has been cited by 4 publications

Distinct longevity mechanisms across and within species and their association with aging [ Cell, 2023, 186(13):2929-2949.e20] PubMed: 37269831
Deguelin suppresses non-small cell lung cancer by inhibiting EGFR signaling and promoting GSK3β/FBW7-mediated Mcl-1 destabilization. [ Cell Death Dis, 2020, 11(2):143] PubMed: 32081857
Identification of Mubritinib (TAK 165) as an inhibitor of KSHV driven primary effusion lymphoma via disruption of mitochondrial OXPHOS metabolism [ Oncotarget, 2020, 11(46):4224-4242] PubMed: 33245718
GPRC5A Is a Negative Regulator of the Pro-Survival PI3K/Akt Signaling Pathway in Triple-Negative Breast Cancer [ Front Oncol, 2020, 10:624493] PubMed: 33680947

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.