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Chemical and physical data
Formula C19H14N2O2S
Molar mass 334.39 g·mol−1
3D model (JSmol)

Tideglusib (NP-12, NP031112) is a potent, selective and irreversible [1] small molecule non-ATP-competitive glycogen synthase kinase 3 (GSK-3) inhibitor.


Other GSK inhibitors

There are few classes of GSK-inhibitors, including lithium (Martinez et al., 2011), the small peptide L803mts10, and members of the thiazolidinedione family, containing non-competitive inhibitors of GSK-3, such as TDZD-8 (Shapira et al., 2007) or Tideglusib® (Noscira, Madrid, and Spain), the latter having an irreversible inhibitory effect on GSK-3 (del Ser et al., 2013). The inhibition of the GSK-3 pathways through distinct mechanisms has been associated with a wide range of adverse reactions, ranging from mild, such as vertigo—or diarrhea (del Ser et al., 2013)—to very severe, such as hypoglycemia—or tumorigenesis (Martinez et al., 2011). The use of Tideglusib specifically was associated with mild-moderate adverse reactions, which included transient increases in serum creatine kinase, ALT—or gGT—diarrhea, nausea, cough, fatigue, and headache (del Ser et al., 2013). In a phase-IIa clinical trial, the treatment was discontinued in 35% of all the active subjects, mainly due to adverse reactions (del Ser et al., 2013).

Potential applications

Tideglusib is under investigation for multiple applications:

Related Research Articles

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GSK3A protein-coding gene in the species Homo sapiens

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PI3K/AKT/mTOR pathway

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