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KI3330SB 21676310 mg$200

Chemical Characteristic

Product NameSB 216763
CAS No.280744-09-4
Molecular Weight 371.21678
FormulaC19H12Cl2N2O2
Chemical Name3-(2,4-dichlorophenyl)-4-(1-methylindol-3-yl)pyrrole-2,5-dione
SmilesN1C(=O)C(=C(C1=O)c1cn(c2c1cccc2)C)c1c(cc(cc1)Cl)Cl
Chemical Structure

Biological activities

SB 216763 is a potent, selective, and ATP-competitive inhibitor of glycogen synthase kinase-3 (GSK-3). The IC50 of SB 216763 against GSK-3α is 34.3 nM. SB 216763 effectively inhibits human GSK-3α and GSK-3β with similar potency. SB 216763 stimulates glycogen synthesis in human liver cells and increases expression of a β-catenin-LEF/TCF regulated reporter gene in HEK293 cells.[1] In vitro, SB 216763 protects both central and peripheral nervous system neurones in culture from death induced by reduced PI 3-kinase (PI3K) pathway activity.[2] SB 216763 also can promotes pluripotency in mouse embryonic stem cells (mESCs) in the absence of exogenous leukemia inhibitory factor (LIF) when cultured on mouse embryonic fibroblasts (MEFs) in vitro.[3] SB 216763 in combination with bleomycin (BLM) prevents lung inflammation and the subsequent fibrosis in mice. Treatment with SB 216763 plus BLM also causes a significant reduction in BLM-induced alveolitis. Moreover, SB 216763 treatment is associated with a significantly lower production of inflammatory cytokines by macrophages.[4] SB 216763 treatment reduces tau phosphorylation (Ser396) in the hippocampus of postnatal rats in vivo.[5]

Protocols

In vitro: SB 216763 is dissolved in DMSO.[5]

References

[1] Coghlan MP, et al. Selective small molecule inhibitors of glycogen synthase kinase-3 modulate glycogen metabolism and gene transcription. Chem Biol. 2000, 7(10): 793-803.
[2] Cross DA, et al. Selective small-molecule inhibitors of glycogen synthase kinase-3 activity protect primary neurones from death. Neurochem. 2001, 77(1): 94-102.
[3] Kirby LA, et al. Glycogen synthase kinase 3 (GSK3) inhibitor, SB-216763, promotes pluripotency in mouse embryonic stem cells. PLoS One. 2012, 7(6): e39329.
[4] Gurrieri C, et al. 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.2010,332(3):785-794.
[5] Selenica ML, et al. Efficacy of small-molecule glycogen synthase kinase-3 inhibitors in the postnatal rat model of tau hyperphosphorylation. Br J Pharmacol. 2007, 152(6): 959-979.

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