Tideglusib (NP031112, NP-12) is a potent non ATP-competitive inhibitor of GSK3 with IC50 of 60 nM.
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Source | Nat Cell Biol (2016). Figure 7. Tideglusib |
| Method | immunoblotting | |
| Cell Lines | GSC11 cells | |
| Concentrations | 2.5 μM or 5 μM | |
| Incubation Time | 36 h | |
| Results | Tideglusib was reported to increase the level of phosphorylated GSK3β-S9, which was also found in GSC11 cells |
| Molecular Weight | 334.39 |
| Formula | C19H14N2O2S |
| CAS Number | 865854-05-3 |
| Solubility (25°C) | DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[3] Teng Yang, et al. Tideglusib and Its Analogues As Inhibitors of Staphylococcus aureus SrtA
[4] Zhiting Chen, et al. Tideglusib, a prospective alternative to nonoxynol-9 contraceptive
| Related GSK-3 Products |
|---|
| Phospho-Glycogen Synthase Peptide-2(substrate)
Phospho-Glycogen Synthase Peptide-2 (substrate) is peptide substrate for glycogen synthase kinase-3 (GSK-3) and can be used for affinity purification of protein-serine kinases. |
| FRATtide
FRATtide is a peptide derived from the GSK-3 binding protein that inhibits the phosphorylation of Axin and β-catenin. |
| ZDWX-25
ZDWX-25 is a highly potent GSK-3β and DYRK1A dual inhibitor with an IC50 value of 71 nM for GSK-3β. |
| TC-G 24
TC-G 24 is a potent, selective glycogen synthase kinase-3β (GSK-3β) inhibitor with an IC50 of 17.1 nM. |
| SAR502250
SAR502250 is a potent, selective, ATP competitive, orally active and brain-penetrant inhibitor of GSK3, with an IC50 of 12 nM for human GSK-3β. |
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