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AdipoGen Life Sciences
TDZD-8
60
CHF
CHF 60.00
In stock
AG-CR1-3740-M0055 mgCHF 60.00
AG-CR1-3740-M02525 mgCHF 130.00
| Product Details | |
|---|---|
| Synonyms | NP 01139; 2-Methyl-4-(phenylmethyl)-1,2,4-thiadiazolidine-3,5-dione |
| Product Type | Chemical |
| Properties | |
| Formula |
C10H10N2O2S |
| MW | 222.3 |
| CAS | 327036-89-5 |
| Purity Chemicals | ≥98% (HPLC) |
| Appearance | White to off-white powder. |
| Solubility | Soluble in DMSO (20mg/ml), DMF (20mg/ml) or ethanol (20mg/ml). |
| Identity | Determined by 1H-NMR. |
| InChi Key | JDSJDASOXWCHPN-UHFFFAOYSA-N |
| Smiles | O=C(N1CC2=CC=CC=C2)N(C)SC1=O |
| Shipping and Handling | |
| Shipping | AMBIENT |
| Short Term Storage | +4°C |
| Long Term Storage | -20°C |
| Handling Advice | Keep cool and dry. |
| Use/Stability | Stable for at least 2 years after receipt when stored at -20°C. |
| Documents | |
| MSDS |
 Download PDF |
| Product Specification Sheet | |
| Datasheet |
Download PDF |
Description
- TDZD-8 is a non-ATP competitive selective inhibitor of the serine/threonine kinase glycogen synthase kinase 3β (GSK3β; IC50 = 2µM), binding to the active site of GSK3β. It does not significantly affect the activities of Cdk-1/cyclin B, CK-II, cAMP-dependent protein kinase or protein kinase C (IC50s = >100 µM), but inhibits PKC and Flt-3 activities (IC50 = 1.4-5.5µM and 673nM, respectively).
- TDZD-8 has been used to study the role of GSK3β during stem cell differentiation as well as in cell and animal models of Alzheimer’s disease and other neurodegenerative disorders.
- TDZD-8 is a potent anti-proliferative and pro-apoptotic agent of glioma cells in vitro and in vivo. These effects are associated with an early activation of extracellular signal-regulated kinase (ERK), which is followed by an increased expression of the early growth response-1 (EGR-1) and p21.
- TDZD-8 potentially inhibits the 33.8-kDa Main protease (Mpro)/3C-like protease of SARS-CoV-2, consequently inhibiting viral transcription and replication and possibly inhibiting spread of COVID-19.
Product References
- First non-ATP competitive glycogen synthase kinase 3 β (GSK-3β) inhibitors: Thiadiazolidinones (TDZD) as potential drugs for the treatment of Alzheimer’s disease: A. Martinez, et al.; J. Med. Chem. 45, 1292 (2002)
- Rapid and selective death of leukemia stem and progenitor cells induced by the compound 4-benzyl, 2-methyl, 1,2,4-thiadiazolidine, 3,5 dione (TDZD-8): M.L. Guzman, et al.; Blood 110, 4436 (2007)
- Treatment with the glycogen synthase kinase-3beta inhibitor, TDZD-8, affects transient cerebral ischemia/ reperfusion injury in the rat hippocampus: M. Collino, et al.; Shock 30, 299 (2008)
- Inhibition of Glioblastoma Growth by the Thiadiazolidinone Compound TDZD-8: D. Aguilar-Morante, et al.; PLoS ONE 5, e13879 (2010)
- GSK-3 inhibitors: Preclinical and clinical focus on CNS: H. Eldar-Finkelman & A. Martinez; Front. Mol. Neurosci. 4, 1 (2011)
- GSK-3β inhibitor TDZD-8 reduces neonatal hypoxic-ischemic brain injury in mice: S. Huang, et al.; CNS Neurosci. Ther. 23, 405 (2017)
- The GSK3β Inhibitor, TDZD-8, Rescues Cognition in a Zebrafish Model of Okadaic Acid-Induced Alzheimer's Disease: D. Koehler, et al.; Neurochem. Int. 122, 31 (2019)
- Structure of Mpro from SARS-CoV-2 and discovery of its inhibitors: Z. Jin, et al.; Nature 582, 289 (2020)
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