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Tocris/SB 216763/1616/1/1 mg

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货号: 1616/1

品牌: Tocris

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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)

Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity

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

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	27.84	75
	ethanol	0.48	1.3

Preparing Stock Solutions

The following data is based on the product molecular weight 371.22. Batch specific molecular weights may vary from batch to batch due to solvent 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

Product Datasheets

Certificate of Analysis / Product Datasheet

Safety Datasheet

References

References are publications that support the products' biological activity.

Coghlan et al (2000) Selective small molecule inhibitors of glycogen synthase kinase-3 modulate glycogen metabolism and gene transcription. Chem.Biol. 7 793 PMID: 11033082

Cross et al (2001) Selective small-molecule inhibitors of glycogen synthase kinase-3 activity protect primary neurones from death. J.Neurochem. 77 94 PMID: 11279265

Gurrieri et 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

Kirby et al (2012) Glycogen synthase kinase 3 (GSK3) inhibitor, SB-216763, promotes pluripotency in mouse embryonic stem cells. PLoS One 7 e39329 PMID: 22745733

Keywords: SB 216763, supplier, Potent, selective, GSK-3, inhibitors, inhibits, Glycogen, Synthase, Kinases, 3, Carbohydrate, Metabolism, SB216763, GlaxoSmithKline, GSK, Glycogen, Synthase, Kinase, 3, Glycogen, Synthase, Kinase, Stem, Cell, Proliferation, Glycogen, Synthase, Kinase, 3, Tocris Bioscience

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