TDZD-8
TDZD-8 is an inhibitor of glycogen synthase kinase 3β (GSK-3β) that exhibits anti-inflammatory, anti-arthritic, and neuroprotective activities. TDZD-8 prevents hemorrhagic shock-induced changes in liver microcirculation and hepatocellular injury, inhibiting the inflammatory response and improving liver function in vivo. In rheumatoid arthritis synoviocytes, TDZD-8 decreases levels of p38 MAPK, ATF-2, c-jun, and JNK; in matched animal models, this compound decreases collagen-induced arthritis by inhibiting infiltration of T cells and macrophages as well as decreasing levels of IL-1β, IL-6, TNF-α, and IFN-γ. In other animal models, TDZD-8 improves deficits in spontaneous alternation in the Y-maze and changes in locomotor activity induced by amphetamines and viral-like immune activation.
References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18974979
| Cas No. |
327036-89-5 |
|---|---|
| Purity |
≥98% |
| Formula |
C10H10N2O2S |
| Formula Wt. |
222.26 |
| Chemical Name |
4-Benzyl-2-methyl-1,2,4-thiadiazolidine-3,5-dione |
| IUPAC Name |
4-benzyl-2-methyl-1,2,4-thiadiazolidine-3,5-dione |
| Melting Point |
63-64.4°C |
| Solubility |
Soluble in DMSO (18mg/mL). |
| Appearance |
White to off white powder |
Jellestad L, Fink T, Pradarutti S, et al. Inhibition of glycogen synthase kinase (GSK)-3-β improves liver microcirculation and hepatocellular function after hemorrhagic shock. Eur J Pharmacol. 2014 Feb 5;724:175-84. PMID: 24389157.
Kwon YJ, Yoon CH, Lee SW, et al. Inhibition of glycogen synthase kinase-3β suppresses inflammatory responses in rheumatoid arthritis fibroblast-like synoviocytes and collagen-induced arthritis. Joint Bone Spine. 2013 Oct 28. [Epub ahead of print]. PMID: 24176738.
Willi R, Harmeier A, Giovanoli S, et al. Altered GSK3β signaling in an infection-based mouse model of developmental neuropsychiatric disease. Neuropharmacology. 2013 Oct;73:56-65. PMID: 23707483.
