SB 415286 Chemische Eigenschaften,Einsatz,Produktion Methoden
R-Sätze Betriebsanweisung:
R36/37/38:Reizt die Augen, die Atmungsorgane und die Haut.
S-Sätze Betriebsanweisung:
S26:Bei Berührung mit den Augen sofort gründlich mit Wasser abspülen und Arzt konsultieren.
S36:DE: Bei der Arbeit geeignete Schutzkleidung tragen.
Beschreibung
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.
Verwenden
SB 415286 was used to treat neuroblastoma cells and study the effect of GSK-3 inhibition on cell proliferation.
Definition
ChEBI: A member of the class of maleimides carrying 3-chloro-4-hydroxyphenylamino and 2-nitrophenyl substituents at positions 3 and 4 respectively.
Biologische Aktivität
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 Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
