Biological Activity
Selective non-ATP competitive inhibitor of GSK 3β (IC50 = 2 μM); thiadiazolidinone deriviative. Does not inhibit Cdk-1/cyclin B, CK-II, PKA or PKC at >100 μM. Reduces severity of L-dopa-induced dyskinesia in a Parkinson's disease in vivo model.
Technical Data
| M. Wt | 222.26 |
| Formula | C10H10N2O2S |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 327036-89-5 |
| PubChem ID | 4124851 |
| InChI Key | JDSJDASOXWCHPN-UHFFFAOYSA-N |
| Smiles | CN1SC(N(C1=O)CC2=CC=CC=C2)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 22.23 | 100 | |
| ethanol | 22.23 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 222.26. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 4.5 mL | 22.5 mL | 44.99 mL |
| 5 mM | 0.9 mL | 4.5 mL | 9 mL |
| 10 mM | 0.45 mL | 2.25 mL | 4.5 mL |
| 50 mM | 0.09 mL | 0.45 mL | 0.9 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Xie et al (2016) Inhibition of Glycogen Synthase Kinase-3β (GSK-3 beta ) as potent therapeutic strategy to ameliorates L-dopa-induced dyskinesia in 6-OHDA parkinsonian rats. Sci.Rep. 6 23527 PMID: 26997328
Martinez et al (2002) First non-ATP competitive glycogen synthase kinase 3 beta (GSK-3beta) inhibitors: thiadiazolidinones (TDZD) as potential drugs for the treatment of Alzheimer's disease. J.Med.Chem. 45 1292 PMID: 11881998
Keywords: TDZD 8, supplier, TDZD8, NP01139, NP_01139, Selective, non-ATP, competitive, inhibitor, GSK, 3, β, L-dopa-induced, dyskinesia, NP, 01139, Glycogen, Synthase, Kinase, 3, Glycogen, Synthase, Kinase, Glycogen, Synthase, Kinase, 3, Tocris Bioscience
