Deguelin

产品编号: T6817 别名:

(-)-cis-Deguelin,鱼藤素,(-)-Deguelin,魚藤素

Deguelin 是一种 PI3K/Akt 抑制剂，是从 Mundulea sericea 家族植物中分离出来的鱼藤酮类化合物。

陶术生物的所有产品和服务仅用于科学研究，我们不为任何个人用途提供产品和服务。

CAS：522-17-8

规格	库存	价格/RMB	数量
{{item.packagingtext}}	{{item.goodshuoqi}}	{{item.moneyunit}} {{item.finalprice}} {{item.pricetext==null\|\|item.pricetext==''?pricetext:item.pricetext}}

生物活性化学信息储存和溶解度信息参考文献引用文献

产品描述

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.

Cas No.

522-17-8

分子式

C23H22O6

分子量

394.423

别名

(-)-cis-Deguelin;鱼藤素;(-)-Deguelin;魚藤素;Deguelin

参考文献

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

引用文献

[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

储存和溶解度

Ethanol:19.7 mg/mL (50 mM)
DMSO:39.4 mg/mL (100 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years

剂量换算 Deguelin 522-17-8

对于各种应用，安全且有效的用药剂量是很有必要的了解更多

体内实验配液计算器

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 g

给药体积 ul

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 +

重置计算

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。

计算器

摩尔计算器可以帮助您计算

制备已知体积和浓度溶液所需的化合物质量
将已知质量的化合物溶解到所需浓度所需的溶液体积
已知质量的化合物在一定体积内形成的溶液的浓度

质量

浓度

体积

分子量

重置计算

稀释计算器可以帮助您计算

制备已知体积和浓度溶液所需的化合物质量
将已知质量的化合物溶解到所需浓度所需的溶液体积
已知质量的化合物在一定体积内形成的溶液的浓度

浓度（起始）

体积（起始）

浓度（终点）

体积（终点）

重置计算

配液计算器可以帮助您计算

重组计算器可帮助您快速计算试剂的体积，以重组您的小瓶。

溶液体积

质量

配液浓度

重置计算

配液计算器可以帮助您计算

输入化合物的化学式以计算其摩尔质量和元素组成
提示：化学式需区分大小写

分子结构式

总分子量

g/mol

重置计算

技术支持

在抑制剂处理说明中可以找到您可能遇到的问题的答案。主题包括如何准备储备溶液，如何存储产品以及基于细胞的测定和动物实验需要特别注意的问题。

Keywords

Autophagy inhibit (-)-cis-Deguelin Deguelin Protein kinase B 鱼藤素 Akt PKB Inhibitor (-)-Deguelin Apoptosis 魚藤素 522-17-8

Deguelin 相关推荐

相关化合物库推荐该产品包含在如下化合物库中：

注册成功

Deguelin

(-)-cis-Deguelin,鱼藤素,(-)-Deguelin,魚藤素

摩尔计算器可以帮助您计算

稀释计算器可以帮助您计算

配液计算器可以帮助您计算

配液计算器可以帮助您计算