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TIDEGLUSIB | TIDEGLUSIB : Irreversible inhibitor of GSK3B, GSK3A
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (0 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
GSK3A
  • INH:29.5 %
    GSK3B (Mutant:WT, C199A)
    • IC50:5 nM
    • IC50:60 nM
      Inhibitor
      up to 1 uM

      Selectivity

      In Vitro Selectivity Assessment
      Potency Assay Off-Target:
      The selectivity of tideglusib was assessed in a panel of 68 kinases at 10 µM. Percent inhibition obs ...

      Potency
      Cellular
      In Vitro

      GSK3A

      Mode of Action: Inhibitor

      Structure-Activity-Relationship data available? Yes

      GSK3B (Mutant:WT, C199A)

      Mode of Action: Inhibitor

      Structure-Activity-Relationship data available? Yes

      DOI Reference: 10.1074/jbc.M111.306472

      Chemical Information

      Molecular Formula C19H14N2O2S
      SMILEs O=c1sn(-c2cccc3ccccc23)c(=O)n1Cc1ccccc1
      InChI 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
      Molecular weight 334.08 Da
      AlogP 3.2622000000000018
      HBond acceptors 4
      HBond donors --
      Atoms 38

      References

      Publications

      Cross References

      Expert Reviews

      by SERP
      (on 24 Apr 2024 )
      Cellular Use Rating
      Tideglusib significantly reduced cell proliferation, viability, and migration of the neuroblastoma cells at 25 micro-molar concentration (PMID: 33030673) but can promote cell proliferation and wound healing...
      by SERP
      (on 30 Apr 2024 )
      Cellular Use Rating
      This is a reported inhibitor of GSK3beta with an irreversible, non-competitive mechanism of action. Despite careful mechanistic work (Domínguez et al 2011) the exact mechanism of inhibition is unclear...
      by SERP+
      (on 17 Jun 2024 )
      Cellular Use Rating
      Tideglusib is a potent GSK-3beta inhibitor but, based on the provided data, clearly lacks selectivity on screened off-target kinases at 10 µM. Additional testing on other off-target kinases as well as...
      Note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars. Read more about our evaluation criteria