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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
References
Vendors
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Probe Summary

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

      Vendors

      Note: This is not an exhaustive list and does not indicate endorsement by the Portal.

      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...
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