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Submit ReviewTDZD 8
Description: Selective non-ATP competitive inhibitor of GSK 3β
Alternative Names: NP 01139
Chemical Name: 2-Methyl-4-(phenylmethyl)-1,2,4-thiadiazolidine-3,5-dione
Purity: ≥98% (HPLC)
Biological Activity for TDZD 8
TDZD 8 is a 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 for TDZD 8
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for TDZD 8
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 22.23 | 100 | |
| ethanol | 22.23 | 100 |
Preparing Stock Solutions for TDZD 8
The following data is based on the product molecular weight 222.26. Batch specific molecular weights may vary from batch to batch due to the degree 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 for TDZD 8
References for TDZD 8
References are publications that support the biological activity of the product.
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
If you know of a relevant reference for TDZD 8, please let us know.
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Keywords: TDZD 8, TDZD 8 supplier, TDZD8, NP01139, NP_01139, Selective, non-ATP, competitive, inhibitor, GSK, 3, β, L-dopa-induced, dyskinesia, NP, 01139, Glycogen, Synthase, Kinase, 6092, Tocris Bioscience
1 Citation for TDZD 8
Citations are publications that use Tocris products. Selected citations for TDZD 8 include:
Coleen M et al (2020) Glycogen synthase kinase-3 inhibition rescues sex-dependent contextual fear memory deficit in human immunodeficiency virus-1 transgenic mice. Br J Pharmacol 177 5658-5676 PMID: 33080056
Do you know of a great paper that uses TDZD 8 from Tocris? Please let us know.
Reviews for TDZD 8
Average Rating: 5 (Based on 1 Review.)
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Great GSK3 inhibitor.
By
Anonymous on 11/25/2021
Assay Type: In Vivo
Species: Mouse
Cell Line/Tissue: Brain
I have used TDZD to inhibit GSK3 in the brain of mice. After the treatment, we investigated if the NCS-1 gene would increase its expression as we have hypothesised the GSK3 protein impairs NCS-1 gene expression. We found that this happened, but only in the pre frontal cortex (PFC) as showed by the figure.
We treated mice with TDZD-8 at 30 mg/kg, i.p. for 1 h
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Pathways for TDZD 8
