Tideglusib

Tideglusib (NP031112) is an irreversible GSK-3 inhibitor with IC₅₀s of 5 nM and 60 nM for GSK-3β^WT (1 h preincubation) and GSK-3β^C199A (1 h preincubation), respectively. IC50 & Target:IC50: 5 nM (GSK-3β^WT), 60 nM (GSK-3β^C199A)^[1] In Vitro:Incubation of both astrocyte and microglial cultures with Tideglusib (NP031112) completely abrogates the induction of TNF-α and COX-2 expression after glutamate treatment. These effects of NP031112 are not caused by a loss of cell viability, because the 24 h exposure of astrocyte and microglial cells to this TDZD does not modify cell viability^[2]. In Vivo:Injection of Tideglusib (NP031112) (50 mg/kg) into the rat hippocampus dramatically 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].