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| SB216763 Basic information |
| Product Name: | SB216763 | | Synonyms: | CS-332;GSK-3 Inhibitor IV, SB-216763 - CAS 280744-09-4 - Calbiochem;SB 216763;3-(2,4-DICHLOROPHENYL)-4-(1-METHYL-1H-INDOL-3-YL)-1H-PYRROLE-2,5-DIONE;3-(2,4-Dichlorophenyl)-4-...;3-(2,4-dichlorophenyl)-4-(1-methyl-1H-indol-3-yl)-2,5-dihydro-1H-pyrrole-2,5-dione;SB-216763(SB 216763);GSK-3 Inhibitor IV, SB-216763 | | CAS: | 280744-09-4 | | MF: | C19H12Cl2N2O2 | | MW: | 371.22 | | EINECS: | | Product Categories: | Inhibitors;Akt;Protein Kinase;Signalling;mTOR;PI3K | | Mol File: | 280744-09-4.mol |
| SB216763 Chemical Properties |
| Melting point | 287-288.6 °C(lit.) | | Boiling point | 598.1±50.0 °C(Predicted) | | density | 1.47±0.1 g/cm3(Predicted) | | storage temp. | -20°C | | solubility | DMSO: 20 mg/mL, soluble | | form | Orange solid | | pka | 7.27±0.60(Predicted) | | color | orange | | Stability: | Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months. |
| Hazard Codes | Xi | | Risk Statements | 36/37/38 | | Safety Statements | 26-36 | | WGK Germany | 3 | | HS Code | 29339900 |
| SB216763 Usage And Synthesis |
| Description | SB-216763 (280744-09-4) is a potent and selective inhibitor of glycogen synthase kinase-1 (GSK-3) IC50=34.3 nM.1 Acts at the ATP-binding domain. Displays protective effects in lung fibrosis mouse model.2 Displays neuroprotective effects on cultured neurons.3 SB-216763 maintains mouse embryonic stem cells in a pluripotent state.4?Cell permeable. | | Uses | SB 216763 is a potent and selective cell permeale ATP-competitive inhibitor of GSK3a. It stimulates glycogen synthesis in Chang human liver cells. | | Uses | SB-216763 was used to inhibit GSK-3β in human brain microvascular endothelial cell line and colorectal cancer cells. | | Biological Activity | Potent and selective glycogen synthase kinase-3 (GSK-3) inhibitor (K i = 9 nM for GSK-3 α ); competes with ATP. Has minimal activity against 24 other protein kinases (IC 50 > 10 μ M). Stimulates glycogen synthesis, gene transcription and is neuroprotective. | | Biochem/physiol Actions | SB-216763 is a small molecule that competes with ATP and potently inhibits the activity α and β isozymes of GSK-3. It acts as neuroprotectant and prevents neuronal cell death induced by PI3-kinase pathway. It also delays preconditioning, reduces infarct size and prevents cardiac ischemia. | | References | 1) Coghlan et al. (2000), Selective small molecule inhibitors of glycogen synthase kinase-3 modulate glycogen metabolism and gene transcription; Chem. Biol., 7 793
2) 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
3) Cross et al. (2001), Selective small-molecule inhibitors of glycogen synthase kinase-3 activity protect primary neurons from death; J. Neurochem., 77 94
4) Kirby et al. (2012), Glycogen synthase kinase 3 (GSK3) inhibitor , SB-216763, promotes pluripotency in mouse embryonic stem cells; PLoS One, 7 e39329 |
| SB216763 Preparation Products And Raw materials |
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