Indirubin-3′-monoxime(Synonyms: Indirubin-3′-oxime)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Indirubin-3′-monoxime (Synonyms: Indirubin-3′-oxime) 纯度: 99.89%

Indirubin-3′-monoxime 是一种有效的 GSK-3β 抑制剂,对 5-Lipoxygenase 的抑制作用较弱,IC50 值分别为 22 nM 和 7.8-10 µM;Indirubin-3′-monoxime 同时对 CDK5/p25 和 CDK1/cyclin B 也有较强作用,IC50 值分别为 100 和 180 nM。

Indirubin-3

Indirubin-3′-monoxime Chemical Structure

CAS No. : 160807-49-8

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥770 In-stock
5 mg ¥700 In-stock
10 mg ¥1100 In-stock
50 mg ¥4400 In-stock
100 mg   询价  
200 mg   询价  

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生物活性

Indirubin-3′-monoxime is a potent GSK-3β inhibitor, and weakly inhibits 5-Lipoxygenase, with IC50s of 22 nM and 7.8-10 µM, respectively; Indirubin-3′-monoxime also shows inhibitory activities against CDK5/p25 and CDK1/cyclin B, with IC50s of 100 and 180 nM.

IC50 & Target[1][3]

GSK-3β

22 nM (IC50)

CDK5/p25

100 nM (IC50)

CDK1/cyclin B

180 nM (IC50)

5-LOX

7.8-10 μM (IC50)

体外研究
(In Vitro)

Indirubin-3′-monoxime inhibits GSK-3β by competing with ATP, with Ki of 0.85 μM, and Km of 110 μM. Indirubin-3′-monoxime also inhibits tau phosphorylation by GSK-3β, with an IC50 value of around 100 nM. Indirubin-3′-monoxime completely inhibits the phosphorylation of the AT100 epitope[1]. Indirubin-3′-monoxime inhibits vascular smooth muscle cell (VSMC) proliferation with IC50 of ∼2 µM. Indirubin-3′-monoxime blunts migration of VSMC stimulated with the PDGF. Indirubin-3′-monoxime interferes with the migratory response in VSMC, and also suppresses the production of pro-migratory LT in monocytes. Moreover, Indirubin-3′-monoxime inhibits 5-lipoxygenase (5-LO) product synthesis in monocytes and neutrophils, with the same potency (IC50=5.0±1.1 and 3.7±1.2 µM, respectively). Indirubin-3′-monoxime is an inhibitor of 5-LO, with IC50 of 7.8-10 µM in cell-free assay[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Indirubin-3′-monoxime (0.1, 0.2 and 0.4 mg/kg, i.p) dose dependently reverses the cognitive impairment and combats the elevated oxidative stress markers in HFD fed mice. Indirubin-3′-monoxime also dose dependently lowers the serum glucose, TGs, TC and insulin levels, and improves the β-cell functioning in HFD fed mice. Moreover, Indirubin-3′-monoxime treatment significantly decreases HOMA-IR levels compared to HFD group. Indirubin-3′-monoxime (0.4 mg/kg) significantly attenuates the increased EL in the HFD group[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

277.28

Formula

C16H11N3O2

CAS 号

160807-49-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 37 mg/mL (133.44 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.6065 mL 18.0323 mL 36.0646 mL
5 mM 0.7213 mL 3.6065 mL 7.2129 mL
10 mM 0.3606 mL 1.8032 mL 3.6065 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (9.02 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (9.02 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
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]. 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):1009-15.

    [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]. Cao Z, et al. Indirubin Derivatives as Dual Inhibitors Targeting Cyclin-Dependent Kinase and Histone Deacetylase for Treating Cancer [published online ahead of print, 2021 Oct 8]. J Med Chem. 2021;10.1021/acs.jmedchem.1c01311.

Kinase Assay
[1]

GSK-3β is expressed in and purified from insect Sf9 cells. It is assayed, following a 1/100 dilution in 1 mg/mL BSA, 10 mM DTT, with 5 μL of 40 μM GS-1 peptide as a substrate, in buffer A, in the presence of 15 μM[γ-32P]ATP (3000 Ci/mmol; 1 mCi/mL) in a final volume of 30 μL. After 30-min incubation at 30°C, 25-μL aliquots of supernatant are spotted onto 2.5×3-cm pieces of Whatman P81 phosphocellulose paper, and, 20 s later, the filters are washed five times (for at least 5 min each time) in a solution of 10 mL of phosphoric acid/liter of water. The wet filters are counted in the presence of 1 mL of ACS scintillation fluid[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[3]

Cytotoxicity of Indirubin-3′-monoxime in monocytes is analysed by MTT assay in a 96-well format using a multi-well scanning spectrophotometer. Neutrophils (5×106 cells/mL) or monocytes (2×106 cells/mL) are incubated for 30 min with Indirubin-3′-monoxime, and the viability of the cells is analysed by MTT assay. Compared with vehicle (0.3% DMSO), no significant acute cytotoxicity is observed (neutrophils: 103.9±4.4%; monocytes: 129.4±5.4%; n=3, each)[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[2]

Male mice (5-6 weeks old) are randomLy assigned into five groups (n=10). Group 1: receive normal pellet diet (NPD); Group 2: receive a HFD; Group 3-5 receive HFD for 8 weeks followed by Indirubin-3′-monoxime treatment (0.1, 0.2 and 0.4 mg/kg i.p, respectively) once daily for 1 week. Indirubin-3′-monoxime is dissolved in (2.5% v/v) DMSO in saline. The mice in NPD and HFD groups receive an equivalent volume of vehicle (2.5% v/v DMSO in saline). Doses of Indirubin-3′-monoxime are selected. Mice are 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 is recorded weekly throughout the experimental period[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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]. 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):1009-15.

    [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]. Cao Z, et al. Indirubin Derivatives as Dual Inhibitors Targeting Cyclin-Dependent Kinase and Histone Deacetylase for Treating Cancer [published online ahead of print, 2021 Oct 8]. J Med Chem. 2021;10.1021/acs.jmedchem.1c01311.

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