货号 | 13621S |
使用方法 | SB216763 is supplied as a lyophilized powder. For a 25 mM stock, reconstitute the 5 mg in 538.8 µl DMSO. Working concentrations and length of treatment can vary depending on the desired effect, but it is typically used at 5-25 µM for 3-24 hr. |
供应商 | CST |
背景 | 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-3α in an ATP competitive manner with an IC50 of 34 nM, and is an equally effective GSK3-β inhibitor. Similar assays demonstrate that SB216763 (at concentrations up to 10 µM) 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 3.6 µM) via glycogen synthase activation and induces expression of a β-catenin regulated reporter gene in HEK293 cells (1). Furthermore, SB216763 induces accumulation of β-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. |
存放说明 | -20C |
纯度 | >98% |
计算分子量 | 371.20 g/mol |
参考文献 | 1 . Coghlan, M.P. et al. (2000) Chem Biol 7, 793-803. 2 . Cross, D.A. et al. (2001) J Neurochem 77, 94-102. 3 . Piazza, F. et al. (2010) BMC Cancer 10, 526. 4 . Zhou, F. et al. (2011) Mol Biol Cell 22, 3533-40. 5 . Gebhardt, R. et al. (2010) J Cell Mol Med 14, 1276-93. |
Chemical structure of SB216763. | |
Western blot analysis of extracts from 293T cells, untreated (-) or treated with SB216763 (4 hr) at the indicated concentrations, using Non-phospho (Active) β-Catenin (Ser33/37/Thr41) (D13A1) Rabbit mAb #8814 (upper), β-Catenin (D10A8) XP® Rabbit mAb #8480 (middle), or β-Actin (D6A8) Rabbit mAb #8457 (lower). |