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SB 216763
CAS No. 280744-09-4
SB 216763( SB-216763 | SB216763 )
Catalog No. M13854 CAS No. 280744-09-4
SB 216763 is a potent, selective, ATP competitive and cell permeable inhibitor GSK-3 with Ki of 9 nM (GSK-3α), equally potent for GSK-3β.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 2MG | 30 | In Stock |
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| 5MG | 43 | In Stock |
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| 10MG | 65 | In Stock |
|
| 25MG | 120 | In Stock |
|
| 50MG | 186 | In Stock |
|
| 100MG | 316 | In Stock |
|
| 500MG | 761 | In Stock |
|
| 1G | Get Quote | In Stock |
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Biological Information
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Product NameSB 216763
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NoteResearch use only, not for human use.
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Brief DescriptionSB 216763 is a potent, selective, ATP competitive and cell permeable inhibitor GSK-3 with Ki of 9 nM (GSK-3α), equally potent for GSK-3β.
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DescriptionSB 216763 is a potent, selective, ATP competitive and cell permeable inhibitor GSK-3 with Ki of 9 nM (GSK-3α), equally potent for GSK-3β; displays no significant activity against a panel of 24 other protein kinases; stimulates glycogen synthesis in human liver cells and induces expression of a beta-catenin-LEF/TCF regulated reporter gene in HEK293 cells, protects both central and peripheral nervous system neurones in culture from death, activates beta-catenin-mediated transcription, and enhances the survival of CLL lymphocytes; displays therapeutic properties in a mouse model of pulmonary inflammation and fibrosis.
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In VitroSB-216763 (10-20 μM) induces β-catenin mediated-transcription in a dose-dependent manner in HEK293 cells. SB-216763 (10, 15 and 20 μM) can maintain mESCs with a pluripotent-like morphology in long-term culture. SB-216763 (10 μM) can maintain J1 mESCs in a pluripotent state for more than a month. SB-216763 inhibits GSK-3 with IC50 of 34 nM. SB-216763 is equally effective at inhibiting human GSK-3α and GSK-3β.
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In VivoSB216763 (20 mg/kg, i.v.) significantly improves the survival of BLM-treated mice. Mice randomized to receive BLM plus SB216763 shows a noteworthy reduction, compared with BLM-treated mice. SB216763 (20 mg/kg, i.v.) reduces the magnitude of BLM-induced alveolitis. SB 216763 (0.2 mg/kg, i.v.) with either 17β-E100 or Geni100 significantly reduce infarct size when the rabbits' hearts are submitted to 30-min CAO.
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SynonymsSB-216763 | SB216763
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PathwayPI3K/Akt/mTOR signaling
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TargetGSK-3
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RecptorGSK-3α|GSK-3β
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Research AreaNeurological Disease
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Indication——
Chemical Information
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CAS Number280744-09-4
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Formula Weight371.2168
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Molecular FormulaC19H12Cl2N2O2
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Purity>98% (HPLC)
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Solubility10 mM in DMSO
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SMILESO=C(C(C1=CC=C(Cl)C=C1Cl)=C2C3=CN(C)C4=C3C=CC=C4)NC2=O
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Chemical Name1H-Pyrrole-2,5-dione, 3-(2,4-dichlorophenyl)-4-(1-methyl-1H-indol-3-yl)-
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Coghlan MP, et al. Chem Biol. 2000 Oct;7(10):793-803.
2. Cross DA, et al. J Neurochem. 2001 Apr;77(1):94-102.
3. Lu D, et al. Proc Natl Acad Sci U S A. 2004 Mar 2;101(9):3118-23.
4. Gurrieri C, et al. J Pharmacol Exp Ther. 2010 Mar;332(3):785-94.
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