靛玉红-3' -单肟 |
| 时间：2023-07-15 来源：化工号 作者：C16H11N3O2 |
| 中文名 | 靛玉红-3' -单肟
| | 英文名 | INDIRUBIN-3'-MONOXIME
| | 别名 | 靛玉红-3
靛玉红-3'-肟
靛玉红-3' -单肟
3-(肟基)-[2,3'-双吲哚啉亚基]-2'-酮
3-(羟基亚氨基)-[2,3'-双吲哚啉亚基]-2'-酮
GSK-3Β抑制剂(INDIRUBIN-3-MONOXIME)
| | 英文别名 | Indirubin-3
INDIRUBIN-3'-OXIME
Indirubine-3'-oxime
INDIRUBIN-3'-MONOXIME
INDIRUBIN-3'-MONOOXIME
3-(hydroxyamino)-1H,2'H-2,3'-biindol-2'-one
3-(Hydroxyimino)-[2,3'-biindolinylidene]-2'-one
3-[1,3-DIHYDRO-3-(HYDROXYIMINO)-2H-INDOL-2-YLIDENE]-1,3-DIHYDRO-2H-INDOL-2-ONE
| | CAS | 160807-49-8
| | 化学式 | C16H11N3O2
| | 分子量 | 277.28 | | InChI | InChI=1/C16H11N3O2/c20-16-13(9-5-1-3-7-11(9)18-16)15-14(19-21)10-6-2-4-8-12(10)17-15/h1-8,17,21H,(H,18,20)/b15-13-,19-14+ | | 密度 | 1.50 | | 熔点 | 247-249°C | | 沸点 | 532.2±50.0 °C(Predicted) | | 水溶性 | DMSO: >10 mg/mL | | 溶解度 | DMSO: >10mg/mL | | 酸度系数 | 8.66±0.20(Predicted) | | 存储条件 | room temp | | 稳定性 | Light Sensitive | | 外观 | solid | | 颜色 | Dark red or brown | | 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 IC 50 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 IC 50 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 (IC 50 =5.0±1.1 and 3.7±1.2 µM, respectively). Indirubin-3'-monoxime is an inhibitor of 5-LO, with IC 50 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. | | WGK Germany | 3 |
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