Antibodies
Tideglusib
- 貨號 Cat. No.
- S2823
- 規格 Size
- 50mgã€200mg
- 品牌 Brand
- Selleckchem
Description
Tideglusib
Catalog No.S28231 Product Citations
Tideglusib is an irreversible, non ATP-competitive GSK-3β inhibitor with IC50 of 60 nM; fails to inhibit kinases with a Cys homologous to Cys-199 located in the active site. Phase 1/2.
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Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw
Biological Activity
| Description | Tideglusib is an irreversible, non ATP-competitive GSK-3β inhibitor with IC50 of 60 nM; fails to inhibit kinases with a Cys homologous to Cys-199 located in the active site. Phase 1/2. | |||||
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| Targets | GSK-3β | |||||
| IC50 | 60 nM [1] | |||||
| In vitro | Tideglusib irreversibly inhibits GSK-3, reduces tau phosphorylation, and prevents apoptotic death in human neuroblastoma cells and murineprimary neurons. [1] Tideglusib (2.5 μM) inhibits glutamate-induced glial activation as evidenced by decreased TNF-α and COX-2 expression in rat primary astrocyte or microglial cultures. Tideglusib (2.5 μM) also exerts a potent neuroprotective effect on cortical neurons from glutamate-induced excitotoxicity as evidenced by significant reduction in the number of Annexin-V-positive cells in rat primary astrocyte or microglial cultures. [2] | |||||
| In vivo | Tideglusib (50 mg/kg) injected into the adult male Wistar rats hippocampus dramatically reduces kainic acid-induced inflammation and has a neuroprotective effect in the damaged areas of the hippocampus. [2]Tideglusib (200 mg/kg, oral) results in lower levels of tau phosphorylation, decreased amyloid deposition and plaque-associated astrocytic proliferation, protection of neurons in the entorhinal cortex and CA1 hippocampal subfield against cell death, and prevention of memory deficits in APP/tau double transgenic mice. [3] | |||||
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Protocol(Only for Reference)
Kinase Assay: [1]
| Binding Experiments with Radiolabeled Tideglusib | [35S]Tideglusib (207 Bq/nmol) at 55 μM is incubated with 5 μM GSK-3β for 1 h at 25 °C in 315 μL of 50 mM Tris-HCl, pH 7.5, containing 150 mM NaCl and 0.1 mM EGTA. The incubation is extended for another 30 min after having added 35 μL of the same buffer with or without 100 mM DTE. Finally, a third 40-μL aliquot of each original sample is mixed with 10 μL of denaturing electrophoresis sample buffer without reducing agents, and 35 μL of this mixture is loaded onto a 10% polyacrylamide gel and subjected to SDS-PAGE, followed by fluorography of the dried gel. |
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Animal Study: [3]
| Animal Models | Transgenic APPsw-tauvlw mice overexpressing human mutant APP and a triple human tau mutation. |
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| Dosages | 200 mg/kg |
| Administration | Oral gavage |
| Solubility | 30% PEG400/0.5% Tween80/5% propylene glycol, 30 mg/mL |
References
Clinical Trial Information( data from http://clinicaltrials.gov)
| NCT Number | Recruitment | Conditions | Sponsor /Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT00948259 | Completed | Alzheimer磗 Disease | Noscira SA | 2008-12 | Phase 1|Phase 2 |
| NCT01049399 | Completed | Progressive Supranuclear Palsy | Noscira SA|i3 Research | 2009-12 | |
| NCT01350362 | Completed | Alzheimers Disease | Noscira SA|ICON Clinical Research | 2011-04 | Phase 2 |
Chemical Information
| Molecular Weight (MW) | 334.39 |
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| Formula | C19H14N2O2S |
| CAS No. | 865854-05-3 |
| Storage | 3 years -20℃Powder |
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| 6 months-80℃in DMSO | |
| Syonnyms | N/A |
| Solubility (25°C) * | In vitro | DMSO | 1 mg/mL (2 mM) |
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| Water | <1 mg/mL (<1 mM) | ||
| Ethanol | <1 mg/mL (<1 mM) | ||
| In vivo | 30% PEG400/0.5% Tween80/5% propylene glycol, | 30 mg/mL | |
| * <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. | |||
| Chemical Name | 1,2,4-Thiadiazolidine-3,5-dione, 2-(1-naphthalenyl)-4-(phenylmethyl)- |
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Product Citations (1)
GSK3 inhibitors regulate MYCN mRNA levels and reduce neuroblastoma cell viability through multiple mechanisms including p53 and Wnt signalling. [Duffy DJ, et al. Mol Cancer Ther 2013;10.1158/1535-7163.MCT-13-0560-T]
PubMed: 24282277
