SB-415286 化学特性,用途語,生産方法
説明
Glycogen synthase kinase 3 (GSK3) is a serine/threonine protein kinase that is inhibited by an assortment of extracellular stimuli such as insulin, growth factors, cell specification factors, and cell adhesion. Its activity regulates many cell functions including the control of cell division, apoptosis, and inflammation. SB-415286 is a potent and selective cell-
permeable, ATP-
competitive inhibitor of GSK3α with an IC
50 value of 78 nM (similar potency for GSK3β) and a K
i value of 31 nM. As a result of GSK3 inhibition, SB-415286 stimulates glycogen synthesis in the Chang human liver cell line with an EC
50 value of 2.9 μM. SB-415286 also protects primary neurons from death induced by the PI3-
kinase pathway.
使用
SB 415286 was used to treat neuroblastoma cells and study the effect of GSK-3 inhibition on cell proliferation.
定義
ChEBI: A member of the class of maleimides carrying 3-chloro-4-hydroxyphenylamino and 2-nitrophenyl substituents at positions 3 and 4 respectively.
生物活性
Potent and selective glycogen synthase kinase-3 (GSK-3) inhibitor (K i = 31 nM for GSK-3 α ); competes with ATP. Has minimal activity against 24 other protein kinases (IC 50 > 10 μ M). Stimulates glycogen synthesis, gene transcription and is neuroprotective.
SB-415286 上流と下流の製品情報
原材料
準備製品