SB 216763

Name: SB 216763
Brand: Tocris Bioscience
SKU: 1616

Tocris Bioscience, part of Bio-Techne | Catalog # 1616

Citations (258)

COA / SDS

Potent, selective GSK-3 inhibitor

Key Product Details

Description:	Potent, selective GSK-3 inhibitor
Chemical Name:	3-(2,4-Dichlorophenyl)-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
Purity:	≥98% (HPLC)
Molecular Weight:	371.22

View Full Technical Details for SB 216763

Technical Data
Citations

Biological Activity for SB 216763

SB 216763 is a 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 >10 μM). 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.

Licensing Information

Sold for research purposes under agreement from GlaxoSmithKline

Technical Data for SB 216763

M. Wt	371.22
Formula	C₁₉H₁₂Cl₂N₂O₂
Storage	Store at RT
Purity	≥98% (HPLC)
CAS Number	280744-09-4
PubChem ID	176158
InChi Key	JCSGFHVFHSKIJH-UHFFFAOYSA-N
Smiles	CN1C=C(C2=CC=CC=C12)C1=C(C(=O)NC1=O)C1=C(Cl)C=C(Cl)C=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for SB 216763

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	37.12	100

Preparing Stock Solutions for SB 216763

The following data is based on the product molecular weight 371.22.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.69 mL	13.47 mL	26.94 mL
5 mM	0.54 mL	2.69 mL	5.39 mL
10 mM	0.27 mL	1.35 mL	2.69 mL
50 mM	0.05 mL	0.27 mL	0.54 mL

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References for SB 216763

References are publications that support the biological activity of the product.

Kirby Glycogen synthase kinase 3 (GSK3) inhibitor, SB-216763, promotes pluripotency in mouse embryonic stem cells. PLoS One 2012 PMID: 22745733
Liang and Chuang Regulation and function of glycogen synthase kinase-3 isoforms in neuronal survival. J.Biol.Chem. 2006 PMID: 17148450
Cross Selective small-molecule inhibitors of glycogen synthase kinase-3 activity protect primary neurones from death. J.Neurochem. 2001 PMID: 11279265
Gurrieri 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 PMID: 19959748
Coghlan Selective small molecule inhibitors of glycogen synthase kinase-3 modulate glycogen metabolism and gene transcription. Chem.Biol. 2000 PMID: 11033082