インジルビン-3'-オキシム 化学特性,用途語,生産方法
説明
Indirubin-
3’-
oxime is a potent inhibitor of glycogen synthase kinase 3β (GSK3β; IC
50 = 22 nM). As GSK3β phosphorylates tau protein, indirubin-
3’-
oxime prevents tau phosphorylation both
in vitro and
in vivo at Alzheimer’s disease-
relevant sites. It also inhibits cyclin-
dependent kinases (CDKs) at higher concentrations, including Cdk1/cyclin B (IC
50 = 180 nM), Cdk2/cyclin A (IC
50 ~500 nM), Cdk2/cyclin E (IC
50 = 250nM), Cdk4/cyclin D1 (IC
50 = 3.3 μM) and Cdk5/p35 (IC
50 = 100 nM). Indirubin-
3’-
oxime reversibly inhibits the proliferation of many cells types, arresting cycling in the G
2/M phase.
化学的特性
Dark Red Solid
使用
A potent inhibitor of GSK-3? (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 (10üM).
生物活性
Protein kinase inhibitor: inhibits cyclin-dependent kinases (IC 50 = 0.18-3.33 μ M) and GSK-3 β (IC 50 = 0.19 μ M). Inhibits CDK5- and GSK-3 β -mediated tau phosphorylation, a process over-active in Alzheimer disease states. Also inhibits AMPK, LCK and SGK. Induces cell cycle arrest and inhibits cell proliferation.
インジルビン-3'-オキシム 上流と下流の製品情報
原材料
準備製品