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Purity: =99.01%
Tideglusib (formerly known as NP031112, NP12) is a novel, potent, irreversible, non-ATP-competitive and chemical inhibitor of GSK-3β (glycogen synthase kinase-3β) with potential neuroprotective effects and may be used as an anti-AD (Alzheimer disease) agent. Tideglusib is presently undergoing phase II clinical trials for Alzheimer's disease and progressive supranuclear palsy; it inhibits GSK-3 with an IC50 of 60 nM in cell-free assay. The lack of recovery in enzyme activity after unbound Tideglusib was removed from the reaction medium and the fact that its dissociation rate constant is not significantly different from zero are evidence that Tideglusib inhibits GSK-3 irreversibly. Additionally, tideglusib was unable to inhibit a number of kinases with an active site Cys homologous to Cys-199, indicating that its inhibition of GSK-3 is the result of a specific mechanism and not nonspecific reactivity.
| Targets |
GSK-3β (IC50 = 5 nM); GSK-3β (IC50 = 60 nM)
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| ln Vitro |
Tideglusib (NP031112) treatment completely eliminates the induction of TNF- and COX-2 expression after glutamate treatment in both astrocyte and microglial cultures. Because the 24-hour exposure of astrocyte and microglial cells to this TDZD has no effect on cell viability, these effects of NP031112 are not brought on by a reduction in cell viability[2].
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| ln Vivo |
Tideglusib (NP031112) (50 mg/kg) injection into the rat hippocampus significantly reduces kainic acid-induced inflammation as measured by edema formation using T2-weighted magnetic resonance imaging and glial activation and has a neuroprotective effect in the damaged areas of the hippocampus[2].
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| Enzyme Assay |
[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. Finally, a third 40-L aliquot of each original sample is combined with 10 L of denaturing electrophoresis sample buffer without reducing agents, and 35 L 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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| Cell Assay |
Cells were treated with indicated concentration of drug for 24 h.
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| Animal Protocol |
Rats; In this study, adult male Wistar rats (8–12 weeks old) are used. Rats (n≥5) are put into a stereotaxic machine. The hippocampus is given an injection of KA (1 μg in 2.5 μL l PBS) alone or in conjunction with Tideglusib (2 ng in 2.5 μL PBS). Animals in the control group are given vehicle injections and are the same age.
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| References |
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| Molecular Formula |
C19H14N2O2S
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|---|---|
| Molecular Weight |
334.3917
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| Exact Mass |
334.0776
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| Elemental Analysis |
C, 68.25; H, 4.22; N, 8.38; O, 9.57; S, 9.59
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| CAS # |
865854-05-3
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| Related CAS # |
865854-05-3
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| Appearance |
Solid powder
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| SMILES |
C1=CC=C(C=C1)CN2C(=O)N(SC2=O)C3=CC=CC4=CC=CC=C43
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| InChi Key |
PMJIHLSCWIDGMD-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H14N2O2S/c22-18-20(13-14-7-2-1-3-8-14)19(23)24-21(18)17-12-6-10-15-9-4-5-11-16(15)17/h1-12H,13H2
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| Chemical Name |
4-benzyl-2-naphthalen-1-yl-1,2,4-thiadiazolidine-3,5-dione
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| Synonyms |
Tideglusib; NP031112, NP-12; NP031112; NP 031112; NP-031112
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~66 mg/mL (~197.4 mM)
Water: <1 mg/mL Ethanol: <1 mg/mL |
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| Solubility (In Vivo) |
4% DMSO+corn oil: 2.5mg/mL (Please use freshly prepared in vivo formulations for optimal results.)
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9905 mL | 14.9526 mL | 29.9052 mL | |
| 5 mM | 0.5981 mL | 2.9905 mL | 5.9810 mL | |
| 10 mM | 0.2991 mL | 1.4953 mL | 2.9905 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Status | Interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05004129 | Recruiting | Drug: Tideglusib | Congenital Myotonic Dystrophy | AMO Pharma Limited | August 23, 2021 | Phase 2 Phase 3 |
| NCT05105958 | Not yet recruiting | Drug: Tideglusib | Amyotrophic Lateral Sclerosis | University Hospital, Geneva | December 1, 2025 | Phase 2 |
| NCT02858908 | Completed | Drug: Tideglusib | Myotonic Dystrophy 1 | AMO Pharma Limited | July 20, 2016 | Phase 2 |
| NCT01350362 | Completed | Drug: tideglusib Drug: Placebo |
Alzheimer's Disease | Noscira SA | April 2011 | Phase 2 |
| NCT00948259 | Completed | Drug: NP031112 Drug: Placebo |
Alzheimer´s Disease | Noscira SA | December 2008 | Phase 1 Phase 2 |
Inhibition of PI3K pathway signaling in cells. KPL-4 cells were treated with the indicated concentrations of CH5132799 for 2 hours. Clin Cancer Res, 2011, 17(10), 3272-3281. |
 Antitumor activity in mouse xenograft models of cell lines harboring genetic alterations, including PIK3CA mutations |
 Antitumor activity in combination with trastuzumab in the trastuzumab-insensitive model. |
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