货号 | 1616/50 |
别名 | 3-(2,4-Dichlorophenyl)-4-(1-methyl- |
供应商 | Tocris |
生物活性 | Potent and selective, ATP-competitive glycogen synthase kinase-3 (GSK-3) inhibitor (IC50 = 34.3 nM for GSK-3α). Equally effective at inhibiting human GSK-3α and GSK-3β. Exhibits minimal activity against 24 other protein kinases (IC50>10μM). Stimulates glycogen synthesis in liver cells, and induces β-catenin-dependent gene transcription. Neuroprotective; also reduces pulmonary inflammation and fibrosis in a mouse model. Shown to maintain mouse embryonic stem cells in a pluripotent state. |
运输条件 | Blue Ice |
存放说明 | Ambient |
纯度 | >98 % |
计算分子量 | 371.22 |
分子式 | C19H12Cl2N2O2 |
可溶性/溶解性 | Soluble to 75 mM in DMSO |
CAS号 | 280744-09-4 |
参考文献 | Kirbyet al (2012) Glycogen synthase kinase 3 (GSK3) inhibitor, SB-216763, promotes pluripotency in mouse embryonic stem cells. PLoS One 7 e39329. PMID: 22745733. Gurrieriet al (2010) 3-(2,4-dichlorophenyl)-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione (SB216763), a glycogen synthase kinase-3 inhibitor, displays therapeutic properties in a mouse model of pulmonary inflammation and fibrosis. J.Pharmacol.Exp.Ther. 332 785. PMID: 19959748. Liang and Chuang (2006) Regulation and function of glycogen synthase kinase-3 isoforms in neuronal survival. J.Biol.Chem. 282 3904. PMID: 17148450. Crosset al (2001) Selective small-molecule inhibitors of glycogen synthase kinase-3 activity protect primary neurones from death. J.Neurochem. 77 94. PMID: 11279265. Coghlanet al (2000) Selective small molecule inhibitors of glycogen synthase kinase-3 modulate glycogen metabolism and gene transcription. Chem.Biol. 7 793. PMID: 11033082. |