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Indirubin-3＇-monoxime

CAS No. : 160807-49-8

MCE 站：Indirubin-3＇-monoxime

产品活性：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。

研究领域：PI3K/Akt/mTOR  |  Stem Cell/Wnt  |  Metabolic Enzyme/Protease

作用靶点：GSK-3  |  Lipoxygenase

In Vitro: 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.

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.

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