TDZD-8

NP 01139; 2-Methyl-4-(phenylmethyl)-124-thiadiazolidine-35-dione

TDZD-8 is a non-ATP competitive selective inhibitor of the serine/threonine kinase glycogen synthase kinase 3? (GSK3?; IC50 = 2?M), binding to the active site of GSK3?. It does not significantly affect the activities of Cdk-1/cyclin B, CK-II, cAMP-dependent protein kinase or protein kinase C (IC50s = >100 ?M), but inhibits PKC and Flt-3 activities (IC50 = 1.4-5.5?M and 673nM, respectively). TDZD-8 has been used to study the role of GSK3? 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.

327036-89-5

C10H10N2O2S

Determined by 1H-NMR.

JDSJDASOXWCHPN-UHFFFAOYSA-N

Lyophilized

222.3

greater than or equal to 98% (HPLC)

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

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

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