靛玉红-3' -单肟
中文名称 | 靛玉红-3' -单肟 |
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中文同义词 | 靛玉红-3' -单肟;靛玉红-3'-肟;靛玉红-3;GSK-3Β抑制剂(INDIRUBIN-3-MONOXIME);3-(羟基亚氨基)-[2,3'-双吲哚啉亚基]-2'-酮;3-(肟基)-[2,3'-双吲哚啉亚基]-2'-酮;INDIRUBIN-3'-MONOXIME (靛玉红-3”-単肟);靛玉红-3'-单肟 |
英文名称 | INDIRUBIN-3'-MONOXIME |
英文同义词 | 3-[1,3-DIHYDRO-3-(HYDROXYIMINO)-2H-INDOL-2-YLIDENE]-1,3-DIHYDRO-2H-INDOL-2-ONE;INDIRUBIN-3'-MONOXIME;INDIRUBIN-3'-OXIME;Indirubine-3'-oxime;INDIRUBIN-3’-MONOOXIME;Indirubin-3;3-(Hydroxyimino)-[2,3'-biindolinylidene]-2'-one;Indirubin-3-monoxime - CAS 160807-49-8 - Calbiochem |
CAS号 | 160807-49-8 |
分子式 | C16H11N3O2 |
分子量 | 277.28 |
EINECS号 | |
相关类别 | 合成;细胞生物学试剂;中药对照品;Intracellular Signaling;Aromatic Hydrazides, Hydrazines, Hydrazones and Oximes;Inhibitors;Protein Kinase |
Mol文件 | 160807-49-8.mol |
结构式 |
靛玉红-3' -单肟 性质
熔点 | 247-249°C |
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沸点 | 532.2±50.0 °C(Predicted) |
密度 | 1.50 |
储存条件 | room temp |
溶解度 | 二甲基亚砜:>10 mg/mL |
形态 | 固体 |
酸度系数(pKa) | 8.66±0.20(Predicted) |
颜色 | 深红色或棕色 |
稳定性 | 感光 |
CAS 数据库 | 160807-49-8 |
Target | Value |
CDK5-P35
(Cell-free assay) | 0.065 μM |
CDK1-cyclinB
(Cell-free assay) | 0.18 μM |
CDK2-cyclinE
(Cell-free assay) | 0.25 μM |
CDK2-cyclinA
(Cell-free assay) | 0.44 μM |
CDK4-cyclinD1
(Cell-free assay) | 3.33 μM |
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.
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.
A potent inhibitor of GSK-3β (IC50=22nM). Also inhibits CDK1 (IC50=180nM) and CDK (IC50=100nM). It reversibly arrests asynchronous HBL-100 cells at G2. It induces apoptosis in the mammary carcinoma cell line MCF-7 (10μM).
安全信息
WGK Germany | 3 |
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提供商 | 语言 |
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英文
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更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2024/04/30 | HY-139254 | 靛玉红-3' -单肟 Indirubin-3′-oxime | 160807-49-8 | 1mg | 500元 |
2024/04/30 | HY-19807 | 靛玉红-3' -单肟 Indirubin-3'-monoxime | 160807-49-8 | 5mg | 500元 |