SB 415286

Описание

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 IC₅₀ 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 EC₅₀ value of 2.9 μM. SB-415286 also protects primary neurons from death induced by the PI3-kinase pathway.

Использование

SB 415286 was used to treat neuroblastoma cells and study the effect of GSK-3 inhibition on cell proliferation.

Определение

ChEBI: A member of the class of maleimides carrying 3-chloro-4-hydroxyphenylamino and 2-nitrophenyl substituents at positions 3 and 4 respectively.

Биологическая активность

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.