Indirubin-3'-monoxime - CAS:160807-49-8

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

目录号 : KM11756 CAS No. : 160807-49-8 纯度 : 98%

Data Sheet 产品使用指南

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。

规格	价格	是否有货
5mg		In-stock
10mg		In-stock
50mg		In-stock
100mg	询价	In-stock
200mg	询价	In-stock

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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.

体外研究

Indirubin-3'-monoxime inhibits GSK-3β by competing with ATP, with K_i of 0.85 μM, and K_m 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.

体内研究

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.

分子式

C₁₆H₁₁N₃O₂

分子量

277.28

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。