Indirubin-3'-monoxime is a powerful inhibitor of GSK-3β with IC50 of 22nM, also inhibits CDK1/5 (IC50 = 180/100 nM).
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HazMat fee for 500 gram (Estimated)
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Indirubin-3'-monoxime is an antagonist to GSK-3β by competing with ATP, displaying a Ki of 0.85 μM, and a Km of 110 μM. Furthermore, it deters the phosphorylation of tau by GSK-3β, showing an IC50 roughly around 100 nM, and fully obstructs the phosphorylation at the AT100 epitope[1]. Additionally, Indirubin-3'-monoxime impedes the proliferation of vascular smooth muscle cells (VSMC) with an IC50 approximately 2 µM. It mitigates the PDGF-induced migration of VSMC and hinders the migratory response in VSMCs, while also diminishing the production of pro-migratory LT in monocytes. Indirubin-3'-monoxime equally curbs the synthesis of 5-lipoxygenase (5-LO) products in monocytes and neutrophils, with IC50 values of 5.0±1.1 and 3.7±1.2 µM, respectively, and it stands as a 5-LO inhibitor with an IC50 between 7.8-10 µM in assays free of cells[3].
Indirubin-3'-monoxime 动物研究
Animal study
Intraperitoneal administration of Indirubin-3'-monoxime (0.1, 0.2, and 0.4 mg/kg) to mice fed on a high-fat diet (HFD) inversely affects cognitive impairment and mitigates elevated markers of oxidative stress. It also reduces the serum levels of glucose, triglycerides (TGs), total cholesterol (TC), and insulin in a dose-dependent manner, enhancing the functionality of β-cells. Furthermore, Indirubin-3'-monoxime notably lowers the HOMA-IR levels compared to those in the HFD group and significantly reduces elevated endogenous lipid (EL) levels in mice on a high-fat diet when administered at 0.4 mg/kg [2].
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