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Indirubin-3'-monoxime

Indirubin-3'-monoxime

产品编号 T5200   CAS 160807-49-8
别名: 靛玉红-3' -单肟, Indirubin-3'-oxime

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。

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Indirubin-3'-monoxime Chemical Structure
Indirubin-3'-monoxime, CAS 160807-49-8
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
其他形式的 Indirubin-3'-monoxime:
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
重组蛋白限时优惠
产品目录号及名称: Indirubin-3'-monoxime (T5200)
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纯度: 99.65%
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生物活性
化学信息
存储 & 溶解度
参考文献
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

存储

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

溶解度

H2O: Insoluble

Ethanol: 15 mg/mL

DMSO: 55 mg/mL (198.36 mM)

溶液配制表

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

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TargetMol Library Books参考文献

1. Leclerc S, et al. Indirubins inhibit glycogen synthase kinase-3 beta and CDK5/p25, two protein kinases involved in abnormal tau phosphorylation in Alzheimer's disease. A property common to most cyclin-dependent kinase inhibitors? J Biol Chem. 2001 Jan 5;276(1):251-60. 2. Damiens E, et al. Anti-mitotic properties of indirubin-3'-monoxime, a CDK/GSK-3 inhibitor: induction of endoreplication following prophase arrest. Oncogene. 2001 Jun 28;20(29):3786-97. 3. Blazevic T, et al. Indirubin-3'-monoxime exerts a dual mode of inhibition towards leukotriene-mediated vascular smooth muscle cell migration. Cardiovasc Res. 2014 Mar 1;101(3):522-32. 4. Sharma S, et al. Neuroprotective role of Indirubin-3'-monoxime, a GSKβ inhibitor in high fat diet induced cognitive impairment in mice. Biochem Biophys Res Commun. 2014 Oct 3;452(4):12009-15.
C-Peptide 1 (rat) Cyanoacetohydrazide GSK3-IN-1 BRD0209 A-674563 GSK-3β inhibitor 3 KY19382 Excisanin A

相关化合物库

该产品包含在如下化合物库中:
抑制剂库 神经退行性疾病化合物库 激酶抑制剂库 抗糖尿病库 代谢化合物库 抗抑郁症化合物库 糖酵解化合物库 抗衰老化合物库 脂代谢化合物库 已知活性化合物库

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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。

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Keywords

Indirubin-3'-monoxime 160807-49-8 Cell Cycle/Checkpoint Metabolism PI3K/Akt/mTOR signaling Stem Cells GSK-3 Lipoxygenase CDK 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

 

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