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Indirubin-3'-oxime

(Synonyms: Indirubin-3'-oxime)
目录号: PC15888 纯度: ≥98%
GSK-3β和CDK抑制剂,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。
CAS No. :160807-49-8
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中文名称
Indirubin-3'-oxime
中文别名
靛玉红-3' -单肟;靛玉红-3''-单肟;2-氨基-2-氟苯甲酮;6,6 -氧代双- 2 -萘磺酸二钠盐;靛玉红-3’-单肟;靛玉红-3-单肟;靛玉红-3;靛玉红-3'-肟;靛玉红-3'-单肟
英文名称
Indirubin-3'-oxime
英文别名
(2E,3E)-3-(Hydroxyimino)-[2,3'-biindolinylidene]-2'-one;INDIRUBIN-3'-OXIME;Indirubin-3-oxime;INDIRUBIN-3'-MONOXIME;INDIRUBIN-3’-MONOOXIME;Indirubin-3’-monoxime;3-[1,3-DIHYDRO-3-(HYDROXYIMINO)-2H-INDOL-2-YLIDENE]-1,3-DIHYDRO-2H-INDOL-2-ONE;Indirubine-3'-oxime;Indirubin-3′-monoxime;Indirubin-3;Indirubin-3'Indirubin-3′INDIRUBIN-3'-OXIME;Indirubin-3monoxime;3-[3-(Hydroxyamino)-1H-indol-2-yl]indol-2-one;Indirubin-3-monoxime;Indirubin 3'-monoxime;indirubin-3'-monooxime;Indirubin-3′-monoxime;(Z)-1H,1'H-[2,3']BIINDOLYLIDENE-3,2'-DIONE-3-OXIME;(2Z,3E)-3-(Hydroxyimino)-[2,3'-biindolinylidene]-2'-one;I
Cas No.
160807-49-8
分子式
C16H11N3O2
分子量
277.28
包装储存
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
详情描述
GSK-3β和CDK抑制剂,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。
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.

性状

Solid

IC50 & Target[1][2]

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. 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.

Medlife 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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature or refrigerated transportation.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
参考文献
溶解度数据
体外研究: 

DMSO : ≥ 37 mg/mL (133.44 mM)

* "≥" means soluble, but saturation unknown.

配制储备溶液
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
*

产品不同,其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液;配成溶液后,建议分装保存,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,建议在 6 个月内使用,-20°C 储存时,建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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.

    建议依照次序添加每种溶剂: 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 ddH?O 中,得到澄清透明的生理盐水溶液
*
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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