|Chemical Name||1,2,4-Thiadiazolidine-3,5-dione, 2-(1-naphthalenyl)-4-(phenylmethyl)-|
|Solubility (25°C) *||In vitro||DMSO||8 mg/mL warmed with 50ºC water bath (23.92 mM)|
|In vivo（should be freshly prepared each time）||4% DMSO+corn oil||2.5mg/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.
|Description||Tideglusib (NP031112, NP-12) is an irreversible, non ATP-competitive GSK-3β inhibitor with IC50 of 60 nM in a cell-free assay; fails to inhibit kinases with a Cys homologous to Cys-199 located in the active site. Phase 2.|
|In vitro||Tideglusib irreversibly inhibits GSK-3, reduces tau phosphorylation, and prevents apoptotic death in human neuroblastoma cells and murineprimary neurons.  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. |
|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.  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. |
|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.|
|Animal Models||Transgenic APPsw-tauvlw mice overexpressing human mutant APP and a triple human tau mutation.|
, , Ann Neurol, 2016, doi: 10.1002/ana.24633
(A) NPCs were treated with 3µM of the GSK3 inhibitor (tideglusib) for 24 hours. Representative images of untreated SPG11-NPCs (SPG11‐NT) and tideglusib-treated SPG11-NPCs (SPG11-Tide) on day 3. Cell proliferation was analyzed using colabeling of PCNA in Nestin/Sox2-positive NPCs. Nuclei were visualized with DAPI. Scale bar = 50µm. (B) Increased numbers of Nestin/Sox2‐positive cells colabeled with PCNA in CHIR99021-treated SPG11-NPCs. (C) Tideglusib-treated SPG11-NPCs, compared to untreated NPCs, revealed restoration of cell proliferation similar to the CTRL‐NPCs.
Data from [Data independently produced by , , Front Immunol, 2018, 9:2527]
BV-2 cells were pretreated with NP-12 (an inhibitor of GSK-3β, 2.5 μM) for 4 h, following which they were treated with PLD for 1 h. After cells were harvested, the protein expression of GSK-3β, p-GSK-3βSer9 (D), and Nucleosol-Nrf2 (E) was measured via Western blotting.
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Sensitivity of pancreatic cancer cells to chemotherapeutic drugs, signal transduction inhibitors and nutraceuticals can be regulated by WT-TP53 [ Adv Biol Regul, 2021, S2212-4926(20)30091-9]PubMed: 33451973
Actionable Cytopathogenic Host Responses of Human Alveolar Type 2 Cells to SARS-CoV-2 [ Mol Cell, 2020, 80(6):1104-1122.e9]PubMed: 33259812
Glycogen synthase kinase 3 β activity is essential for Polo-like kinase 2- and Leucine-rich repeat kinase 2-mediated regulation of α-synuclein. [ Neurobiol Dis, 2020, 136:104720]PubMed: 31881263
GSK-3β Contributes to Parkinsonian Dopaminergic Neuron Death: Evidence From Conditional Knockout Mice and Tideglusib [ Front Mol Neurosci, 2020, 13:81]PubMed: 32581704
Pharmacologic and genetic approaches define human pancreatic β cell mitogenic targets of DYRK1A inhibitors. [ JCI Insight, 2020, 5(1)]PubMed: 31821176
Bidirectional Regulation between NDRG1 and GSK3β Controls Tumor Growth and Is Targeted by Differentiation Inducing Factor-1 in Glioblastoma. [ Cancer Res, 2020, 80(2):234-248]PubMed: 31723002
TRAF6 Inhibits Colorectal Cancer Metastasis Through Regulating Selective Autophagic CTNNB1/β-catenin Degradation and Is Targeted for GSK3B/GSK3β-mediated Phosphorylation and Degradation [ Autophagy, 2019, 15(9):1506-1522]PubMed: 30806153
Tideglusib, a prospective alternative to nonoxynol-9 contraceptive [ Contracept X, 2019, 1:100007]PubMed: 32550526
Suppression of glioblastoma by a drug cocktail reprogramming tumor cells into neuronal like cells. [ Sci Rep, 2019, 9(1):3462]PubMed: 30837577
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