TDZD-8
| Code | Size | Price |
|---|
| AG-CR1-3740-M005 | 5 mg | £65.00 |
Quantity:
| AG-CR1-3740-M025 | 25 mg | £105.00 |
Quantity:
Prices exclude any Taxes / VAT
Overview
Regulatory Status: RUO
Documents
Further Information
Alternate Names/Synonyms:
NP 01139; 2-Methyl-4-(phenylmethyl)-1,2,4-thiadiazolidine-3,5-dione
Appearance:
White to off-white powder.
CAS:
327036-89-5
EClass:
32160000
Form (Short):
liquid
GHS Symbol:
GHS08
Handling Advice:
Keep cool and dry.
Hazards:
H334
InChi:
InChI=1S/C10H10N2O2S/c1-11-9(13)12(10(14)15-11)7-8-5-3-2-4-6-8/h2-6H,7H2,1H3
InChiKey:
JDSJDASOXWCHPN-UHFFFAOYSA-N
Long Description:
Chemical. CAS: 327036-89-5. Formula: C10H10N2O2S. MW: 222.3. TDZD-8 is a non-ATP competitive selective inhibitor of the serine/threonine kinase glycogen synthase kinase 3beta (GSK3beta; IC50 = 2µM), binding to the active site of GSK3beta. 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 GSK3beta 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.
MDL:
MFCD04973552
Molecular Formula:
C10H10N2O2S
Molecular Weight:
222.3
Package Type:
Vial
Precautions:
P304+P340
Product Description:
TDZD-8 is a non-ATP competitive selective inhibitor of the serine/threonine kinase glycogen synthase kinase 3beta (GSK3beta; IC50 = 2µM), binding to the active site of GSK3beta. 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 GSK3beta 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.
Purity:
>98% (HPLC)
Signal word:
Danger
SMILES:
O=C(N1CC2=CC=CC=C2)N(C)SC1=O
Solubility Chemicals:
Soluble in DMSO (20mg/ml), DMF (20mg/ml) or ethanol (20mg/ml).
Transportation:
Non-hazardous
UNSPSC Category:
Biochemical Reagents
UNSPSC Number:
12352200
Use & Stability:
Stable for at least 2 years after receipt when stored at -20°C.
References
First non-ATP competitive glycogen synthase kinase 3 beta (GSK-3beta) 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-3beta inhibitor TDZD-8 reduces neonatal hypoxic-ischemic brain injury in mice: S. Huang, et al.; CNS Neurosci. Ther. 23, 405 (2017) | The GSK3beta 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)