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Deguelin

SKU: orb1300439

Description

Deguelin

Research Area

Cell Biology, Signal Transduction

Images & Validation

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Deguelin

Key Properties

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CAS Number522-17-8
MW394.42
Purity99.29%
FormulaC23H22O6
SMILESCOc1cc2OC[C@H]3Oc4c(ccc5OC(C)(C)C=Cc45)C(=O)[C@H]3c2cc1OC
TargetApoptosis,Autophagy,Akt,PI3K
Solubility10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.07 mM);Ethanol:19.7 mg/mL (49.95 mM);DMSO:252.5 mg/mL (640.18 mM)

Bioactivity

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In Vivo
In pre-clinical trials, deguelin markedly decreased the tumor incidence. It exhibited significant anti-tumorigenesis and anti-proliferative activity in various types of cancer both in vitro and in vivo. Topically-administered deguelin significantly suppressed the multiplicity of skin tumors with UVB-induction, indicating its effect as a potential cancer chemopreventive agent. Treatment with deguelin, a potential mitochondria complex I inhibitor, reduced tyrosine hydroxylase-positive neurons, leading to Parkinson's disease.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.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. 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.
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In Vitro
In leukaemia cell lines, Deguelin downregulates Akt phosphorylation through activating PI3K/Akt axis. Deguelin increases the sensitivity of human leukaemia cells to chemotherapeutic drugs. In U937 cells deguelin does not affect the expression or the phosphorylation levels of either p44/42 or p38 MAP kinases. 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.Deguelin （10 or 100 nmol/l） is potent in inhibiting Akt phosphorylation,while deguelin does not affect total Akt expression. Deguelin dephosphorylates Akt and increases cytarabine sensitivity of AML blasts but not of CB CD34+.
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Cell Research
U937 Cells are incubated with the indicated concentrations (1 nM, 10 nM, 100 nM) of deguelin for 24 h.Flow cytometric analysis of cell cycle in response to deguelin. Flow cytometric analysis of cell cycle in response to deguelin.
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Animal Research
A/J mice were treated by oral gavage of 5.0 or 10.0 mg/kg deguelin dissolved in corn oil.

Storage & Handling

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Storagestore at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

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PI3K, Autophagy, Apoptosis, Akt, (-)-Deguelin, Deguelin, cis-Deguelin

Similar Products

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  • Deguelin

    Deguelin [orb1222118]

    >98% (HPLC)

    522-17-8

    394.42

    C23H22O6

    500 mg, 5 mg, 25 mg, 100 mg, 50 mg, 200 mg, 1 g, 10 mg
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Compound Identifiers

PubChem CID
107935 ↗

Key Properties

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No computed properties available.

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Deguelin (orb1300439)

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% DMSO +
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% Tween 80 +
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1 ml x 10 mM (in DMSO)
$ 90.00
5 mg
$ 90.00
10 mg
$ 120.00
25 mg
$ 180.00
50 mg
$ 310.00
100 mg
$ 480.00
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