靛玉红-3' -单肟

生物活性靶点体外研究体内研究靛玉红-3' -单肟试剂级价格

靛玉红-3' -单肟

CAS号:160807-49-8
英文名:INDIRUBIN-3'-MONOXIME
中文名:靛玉红-3' -单肟
CBNumber:CB1325944
分子式:C16H11N3O2
分子量:277.28
MOL File:160807-49-8.mol

靛玉红-3' -单肟化学性质

熔点 :247-249°C
沸点 :532.2±50.0 °C(Predicted)
密度 :1.50
储存条件 :room temp
溶解度 :DMSO: >10 mg/mL
形态 :solid
酸度系数(pKa) :8.66±0.20(Predicted)
颜色 :Dark red or brown
稳定性 :Light Sensitive
CAS 数据库 :160807-49-8

安全信息

WGK Germany :3

靛玉红-3' -单肟性质、用途与生产工艺

生物活性 Indirubin-3'-monoxime (Indirubin-3'-oxime)是一种选择性的CDK抑制剂，对CDK1-cyclinB, CDK2-cyclinA, CDK2-cyclinE, CDK4-cyclinD1, CDK5-p35的IC50分别为 0.18 μM, 0.44 μM, 0.25 μM, 3.33 μM, 0.065 μM。Indirubin-3'-monoxime是一种直接、选择性的5-lipoxygenase抑制剂，IC50为7.8-10 µM。

靶点

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

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.
用途
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).