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Deguelin

产品编号 T6817 CAS 522-17-8

别名: 鱼藤素, (-)-Deguelin, (-)-cis-Deguelin, 魚藤素

Deguelin ((-)-Deguelin) 是一种 PI3K/AKT 抑制剂，从 Mundulea sericea 家族植物中分离出来的鱼藤酮类天然产物。

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Deguelin, CAS 522-17-8

规格	价格/CNY	货期
5 mg	￥ 339	现货
10 mg	￥ 627	现货
25 mg	￥ 1,398	现货
50 mg	￥ 2,537	现货
100 mg	￥ 3,997	现货
1 mL * 10 mM (in DMSO)	￥ 339	现货

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纯度: 98.26%

纯度: 96.39%

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天然产物信息

生物活性

化学信息

存储 & 溶解度

TCMIP信息

参考文献

相关产品

植物来源	天然产物 > 豆科 > 鱼藤属

产品描述	Deguelin ((-)-Deguelin) is a PI3K/AKT Inhibitor, which is a natural product isolated from plants in the Mundulea sericea family.
体外活性	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+.
体内活性	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.
激酶实验	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).
细胞实验	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.
动物实验	A/J mice were treated by oral gavage of 5.0 or 10.0 mg/kg deguelin dissolved in corn oil.

别名	鱼藤素, (-)-Deguelin, (-)-cis-Deguelin, 魚藤素
分子量	394.42
分子式	C23H22O6
CAS No.	522-17-8

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

Ethanol: 19.7 mg/mL (50 mM)

DMSO: 39.4 mg/mL (100 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
Ethanol / DMSO	1 mM	2.5354 mL	12.6768 mL	25.3537 mL	63.3842 mL
	5 mM	0.5071 mL	2.5354 mL	5.0707 mL	12.6768 mL
	10 mM	0.2535 mL	1.2677 mL	2.5354 mL	6.3384 mL
	20 mM	0.1268 mL	0.6338 mL	1.2677 mL	3.1692 mL
	50 mM	0.0507 mL	0.2535 mL	0.5071 mL	1.2677 mL
DMSO	100 mM	0.0254 mL	0.1268 mL	0.2535 mL	0.6338 mL

TCMIP相关数据

中药材来源及性味归经

中药材名称	中药材拉丁名	性	味	归经
灰叶根	Tephrosia purpurea(L.)Pers.	凉	微苦	脾, 胃
铃兰	Convallaria keiskei Miq.	温	甘, 苦
毛鱼藤	Derris elliptica (Roxb.) Benth.	-	―
木榄	Bruguiera gymnorhiza (Linnaeus) Savigny	平	涩	大肠
鱼藤	Derris trifoliata	温	苦, 辛	肝

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Bortul R, et al. Br J Haematol. 2005, 129(5):677-86. 2. Kim JH, et al. J Pharmacol Exp Ther. 2008, 324(2):643-7. 3. Wang Y, et al. Mol Clin Oncol. 2013, 1(2):215-219. 4. Yan Y, et al. Neoplasia. 2005, 7(12):1053-7.

文献引用

1. Liu X, Yang J, Yang C, et al. Morphine promotes the malignant biological behavior of non-small cell lung cancer cells through the MOR/Src/mTOR pathway. Cancer Cell International. 2021, 21(1): 1-14 2. Liu X, Yang J, Yang C, et al. Morphine promotes the malignant biological behavior of non-small cell lung cancer cells through the MOR/Src/mTOR pathway. Cancer cell International. 2021, 21(1): 1-14

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Deguelin 522-17-8 Apoptosis Autophagy Cytoskeletal Signaling PI3K/Akt/mTOR signaling Akt PI3K inhibit Protein kinase B cis-Deguelin 鱼藤素 PKB (-)-Deguelin Inhibitor (-)-cis-Deguelin 魚藤素 inhibitor

我们的所有产品和服务仅用于科学研究，不能被用于人体，我们也不向个人提供产品和服务。

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Deguelin

存储

溶解度

溶液配制表

中药材来源及性味归经

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

文献引用

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords