Cat. No. 1616
Chemical Name: 3-(2,4-Dichlorophenyl)-4-(1-methyl-
Biological ActivityPotent 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 InformationSold for research purposes under agreement from GlaxoSmithKline
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.
Certificate of Analysis / Safety Data Sheet
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.
Liang and Chuang (2006) Regulation and function of glycogen synthase kinase-3 isoforms in neuronal survival. J.Biol.Chem. 282 3904. PMID: 17148450.
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.
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.
If you know of a relevant citation for this product please let us know.
View Related Products by Target
Keywords: SB 216763, supplier, Potent, selective, GSK-3, inhibitors, Glycogen, Synthase, Kinases, 3, Carbohydrate, Metabolism, SB216763, GlaxoSmithKline, GSK
Find multiple products by catalog number
New Products in this Area
Selective PFKFB3 inhibitorPD 0332991 isethionate
Potent, selective Cdk4/6 inhibitor; brain penetrantXL 413 hydrochloride
Potent and selective Cdc7 inhibitorC16
PKR inhibitorRp-8-pCPT-cGMPS sodium
PKG inhibitorTC-S 7004
Potent and selective DYRK1A/B inhibitorTAK 960 hydrochloride
Potent and selective PLK1 inhibitorA12B4C3
Potent and selective polynucleotide kinase/phosphatase (PKNP) inhibitorBMS 345541
Selective allosteric inhibitor of IKK; anti-inflammatoryWH-4-023
Potent and selective Lck and Src inhibitor; also inhibits SIKTC-S 7006
Potent and selective Tpl2 (Cot; MAP3K8) inhibitorOXA 06 dihydrochloride
Potent ROCK inhibitorPCI 29732
Potent BTK inhibitorMps1-IN-1 dihydrochloride
Selective monopolar spindle 1 (Mps1) kinase inhibitorCKI 7 dihydrochloride
CK1 inhibitorT 5601640
Selective LIMK2 inhibitor; antitumor3PO
PFKFB3 inhibitor; antiangiogenicCHR 6494 trifluoroacetate
Potent and selective haspin kinase inhibitorUNC 3230
Potent and selective PIP5K1C inhibitor; antinociceptivetrans-ISRIB
Integrated stress response (ISR) inhibitorBMS 509744
Potent and selective ITK inhibitor
July 4 - 9, 2015