Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Indirubin-3'-monoxime (Indirubin-3'-oxime) 是一种有效的 GSK3β 抑制剂,IC50值为 22 nM。它对 CDK5/p25、CDK1/cyclin B 和CDk2/cyclin E 也有作用,IC50值分别为 100、180 和 250 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 186 | 现货 | ||
5 mg | ¥ 413 | 现货 | ||
10 mg | ¥ 662 | 现货 | ||
25 mg | ¥ 1,430 | 现货 | ||
50 mg | ¥ 2,650 | 现货 | ||
100 mg | ¥ 3,880 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 455 | 现货 |
产品描述 | Indirubin-3'-monoxime (Indirubin-3'-oxime) is a potent inhibitor of GSK3β (IC50: 22 nM) and also inhibits CDKs ( (IC50s: 100/180/250 nM for Cdk5/p35, Cdk1/cyclin B, Cdk2/cyclin E). |
靶点活性 | CDK2-CyclinE:250 nM (cell free), CDK5-p25:100 nM (cell free), CDK1-CyclinB:180 nM (cell free), GSK-3β:22 nM (cell free) |
体外活性 | Indirubins are powerful inhibitors (IC50: 5-50 nM) of GSK-3 beta. Bacterially expressed recombinant human tau was indeed phosphorylated in vitro by GSK-3β, and this phosphorylation was inhibited in a dose-dependent manner by indirubin-3′-monoxime, with an IC50 value of around 100 nM [1]. Indirubin-3'-monoxime reversibly arrests asynchronous HBL-100 cells in G2. Indirubin-3'-monoxime inhibits the phosphorylation of consensus CDK phosphorylation sites as well as of nucleolin at a specific CDK1/cyclin B phosphorylation site [2]. In cell-based and cell-free assays, Indirubin-3'-monoxime selectively inhibited 5-lipoxygenase (5-LO), the key enzyme in LT biosynthesis, with an IC50 in the low micromolar range [3]. |
体内活性 | The mice treated with IMX showed a significant reduction in plasma glucose, triglycerides, cholesterol, insulin levels and improvement in learning and memory performance, attenuated the oxidative stress and AChE activity. Moreover, IMX dose-dependently augments the brain insulin and BDNF levels in HFD fed mice [4]. |
激酶实验 | Kinase activities were assayed in Buffer A or C (unless otherwise stated), at 30?°C, at a final ATP concentration of 15 μM. Blank values were subtracted, and activities were calculated as picomoles of phosphate incorporated for a 10-min incubation. The activities are usually expressed in percentage of the maximal activity, i.e. in the absence of inhibitors. Controls were performed with appropriate dilutions of dimethyl sulfoxide. In a few cases, phosphorylation of the substrate was assessed by autoradiography after SDS-PAGE [1]. |
细胞实验 | To determine the effects of aminopurvalanol and indirubin-3′-monoxime on tau phosphorylation, Sf9 cells infected with baculovirus expressing htau23 protein were treated 36 h post-infection (when cells have already expressed levels of tau sufficient for the outgrowth of cell processes) with 20 μM inhibitors for 3 h before being harvested [1]. |
动物实验 | Male mice (5–6 weeks old) were randomly assigned into five groups (n = 10). Group 1: received normal pellet diet (NPD); Group 2: received a HFD; Group 3–5 received HFD for 8 weeks followed by Indirubin-3'-monoxime (IMX) treatment (0.1, 0.2 and 0.4 mg/kg i.p, respectively) once daily for 1 week. IMX was dissolved in (2.5% v/v) DMSO in saline. The mice in NPD and HFD groups received an equivalent volume of vehicle (2.5% v/v DMSO in saline). The composition of HFD was similar as described by Srinivasan. Doses of IMX were selected based on the reports available in literature. Mice were kept under standard husbandry conditions (22 ± 1 C and 60% humidity) and maintained on a 12/12-h light/dark schedule with free access to food and water for 8 weeks. Body weight was recorded weekly throughout the experimental period [4]. |
别名 | 靛玉红-3' -单肟, Indirubin-3'-oxime |
分子量 | 277.28 |
分子式 | C16H11N3O2 |
CAS No. | 160807-49-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: Insoluble
Ethanol: 15 mg/mL
DMSO: 55 mg/mL (198.36 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 3.6065 mL | 18.0323 mL | 36.0646 mL | 90.1616 mL |
5 mM | 0.7213 mL | 3.6065 mL | 7.2129 mL | 18.0323 mL | |
10 mM | 0.3606 mL | 1.8032 mL | 3.6065 mL | 9.0162 mL | |
20 mM | 0.1803 mL | 0.9016 mL | 1.8032 mL | 4.5081 mL | |
50 mM | 0.0721 mL | 0.3606 mL | 0.7213 mL | 1.8032 mL | |
100 mM | 0.0361 mL | 0.1803 mL | 0.3606 mL | 0.9016 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
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。
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。
Indirubin-3'-monoxime 160807-49-8 Cell Cycle/Checkpoint Metabolism PI3K/Akt/mTOR signaling Stem Cells Lipoxygenase CDK GSK-3 Indirubin 3' monoxime 靛玉红-3' -单肟 LOX Indirubin-3'-oxime inhibit Indirubin3'monoxime Inhibitor Glycogen synthase kinase-3 Glycogen synthase kinase 3 Cyclin dependent kinase inhibitor