TDZD-8 | 11-080

TDZD-8 | 11-080 | Gentaur UK, US & Europe Distribution

BNR: Chemical

Predicted Molecular Weight: 222, 3

Physical State: Lyophilized

Storage Condition: Short Term Storage: +4C. Long Term Storage: -20C. Handling Advice: Keep cool and dry. Use/Stability: Stable for at least 2 years after receipt when stored at -20C.

Alternate Name: NP 01139; 2-Methyl-4- (phenylmethyl) -1, 2, 4-thiadiazolidine-3, 5-dione

Background: 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.

Disclaimer: This product is for research use only.

Purity: greater than or equal to 98% (HPLC)

Formula: C10H10N2O2S

Source: N/A

Solubility: Soluble in DMSO (20mg/ml), DMF (20mg/ml) or ethanol (20mg/ml) .

InChi Key: JDSJDASOXWCHPN-UHFFFAOYSA-N

Smiles: O=C (N1CC2=CC=CC=C2) N (C) SC1=O

RTECS: N/A

Identity: Determined by 1H-NMR.

Merck Index: N/A