Tideglusib

Tideglusib is a thiadiazolidinone that prevents inflammation and neurodegeneration when injected into rat hippocampus concurrently with kainic acid, a compound that causes excitotoxicity.¹ Tideglusib-induced neuroprotection, in this model, is attenuated by the PPARγ antagonist GW9662 (Item No. 70785).¹ Interestingly, tideglusib also irreversibly inhibits glycogen synthase kinase-3β (GSK3β) with an IC₅₀ value of 5 nM when used with a one hour preincubation, increasing to 0.1-1 µM without preincubation.^2,3 Several GSK3 inhibitors, including tideglusib, promote hippocampal neurogenesis both in vitro and in vivo, suggesting suitability in Alzheimer’s therapy.^3,4

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1. Luna-Medina, R., Cortes-Canteli, M., Sanchez-Galiano, S., et al. NP031112, a thiadiazolidinone compound, prevents inflammation and neurodegeneration under excitotoxic conditions: Potential therapeutic role in brain disorders. J. Neurosci. 27(21), 5766-5776 (2007).

2. Domínguez, J.M., Fuertes, A., Orozco, L., et al. Evidence for irreversible inhibition of glycogen synthase kinase-3β by tideglusib. The Journal of Biological Chemisty 287(2), 893-904 (2012).

3. Morales-Garcia, J.A., Luna-Medina, R., Alonso-Gil, S., et al. Glycogen synthase kinase 3 inhibition promotes adult hippocampal neurogenesis in vitro and in vivo. ACS Chem. Neurosci. 3(11), 963-971 (2012).

4. Martinez, A., Gil, C., and Perez, D.I. Glycogen synthase kinase 3 inhibitors in the next horizon for Alzheimer’s disease treatment. Int. J. Alzheimers Dis. 280502 (2011).