The maleimide derivative SB216763 is a potent and selective cell permeable inhibitor of glycogen synthase kinase 3 (GSK-3). Research studies using peptide-based protein kinase assays show that SB216763 inhibits GSK-3alpha in an ATP competitive manner with an IC50 of 34nM, and is an equally effective GSK3-B inhibitor. Similar assays demonstrate that SB216763 (at concentrations up to 10uM) does not inhibit as many as 24 other serine/threonine and tyrosine protein kinases (1). As a consequence of inhibiting GSK-3, SB216763 stimulates glycogen synthesis in human liver cells (EC50 3.6uM) via glycogen synthase activation and induces expression of a B-catenin regulated reporter gene in HEK293 cells (1). Furthermore, SB216763 induces accumulation of B-catenin, a key downstream effector in the Wnt signaling pathway, in many cell types (2-5). Additional research indicates that SB216763 can prevent neuronal cell death induced by PI3 kinase pathway inhibition (2). Glycogen synthase kinase 3 inhibitors such as SB216763 can be important research tools in studying the functional role of GSK-3 in cell signaling pathways.
Formula:C19H12Cl2N2O2
Solubility:Soluble in DMSO at 20mg/ml. Very poorly soluble in ethanol and water.
Molecular Weight:371.2g/mol
Storage and Stability:Store at -20°C. For maximum recovery of product, centrifuge the original vial prior to removing the cap.
仕様
Size：5mg
Grade：Highly Purified
Purity：Highly Purified (~98%)
Form：Supplied as a lyophilized powder. For a 25mM stock, reconstitute the 5mg in 538.8ul DMSO.
