Deguelin

製品コードS8132 バッチS813201

印刷

化学情報

Chemical Structure Synonyms (-)-Deguelin, (-)-cis-Deguelin Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C23H22O6
分子量 394.42 CAS No. 522-17-8
Solubility (25°C)* 体外 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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Deguelin, a natural product isolated from plants in the Mundulea sericea family, is an PI3K/AKT Inhibitor.
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].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 U937 cells
濃度 1 nM, 10 nM, 100 nM
反応時間 24 h
実験の流れ 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%.
動物実験 動物モデル A/J mice
投薬量 5.0 or 10.0 mg/kg
投与方法 by gavage

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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