TDZD-8 is a serine/threonine glycogen synthase kinase 3beta (GSK-3beta) inhibitor. GSK-3beta is abundant in the central nervous system, particularly in the hippocampus, and plays a pivotal role in the pathophysiology of a number of diseases, including neurodegeneration. TDZD-8 protects the brain against I/R injury by inhibiting GSK-3beta activity. TDZD-8 decreased proliferation and induced apoptosis of GL261 glioblastoma cells in vitro, delayed tumor growth in vivo, and augmented animal survival. These effects were associated with an early activation of extracellular signal-regulated kinase (ERK) pathway and increased expression of EGR-1 and p21 genes.
CAS Number: 327036-89-5
Molecular Weight: 222.26
GSK3 Inhibitor I
Chemical Name: 4-benzyl-2-methyl-1,2,4-thiadiazolidine-3,5-dione
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: Soluble in DMSO, not in water
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥360 days if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
TDZD8 results in a significant decline of cellular ATP levels in PC-3 cells. TDZD8 (10 μM) treatment also triggers a drastic autophagy response and AMPK activation in PC-3 cells. Furthermore, TDZD8 (10 μM) reduces mTOR phosphorylation levels at the S2448 site. In addition, TDZD8 (10 μM) induces LKB1 nuclear-cytoplasm translocation.
TDZD-8 (TDZD8, 1 or 2 mg/kg, i.p.) both reduces the induction of p-DARPP32 following chronic L-dopa treatment in parkinsonian animals. TDZD8 treatment of 21 days induces a significant reduction in PKA expression in rats with established dyskinesia. Moreover, TDZD8 reduces FosB mRNA level in the striatum and lowers the expression of PPEB mRNA to similar levels as in 6-OHDA-lesioned rats without treated with L-dopa. The decrease in dyskinesia induced by TDZD8 is overcome by dopamine rceptor-1 agonist.
- Ansaldi D, Hod EA, Stellari F, Kim JB, Lim E, Roskey M, Francis KP, Singh R, Zhang N. Imaging pulmonary NF-kappaB activation and therapeutic effects of MLN120B and TDZD-8. PLoS One. 2011;6(9):e25093. doi: 10.1371/journal.pone.0025093. Epub 2011 Sep 22. PubMed PMID: 21966423; PubMed Central PMCID: PMC3178604.
- Aguilar-Morante D, Morales-Garcia JA, Sanz-SanCristobal M, Garcia-Cabezas MA, Santos A, Perez-Castillo A. Inhibition of glioblastoma growth by the thiadiazolidinone compound TDZD-8. PLoS One. 2010 Nov 8;5(11):e13879. doi: 10.1371/journal.pone.0013879. PubMed PMID: 21079728; PubMed Central PMCID: PMC2975629.
- Collino M, Thiemermann C, Mastrocola R, Gallicchio M, Benetti E, Miglio G, Castiglia S, Danni O, Murch O, Dianzani C, Aragno M, Fantozzi R. Treatment with the glycogen synthase kinase-3beta inhibitor, TDZD-8, affects transient cerebral ischemia/reperfusion injury in the rat hippocampus. Shock. 2008 Sep;30(3):299-307. doi: 10.1097/SHK.0b013e318164e762. PubMed PMID: 18323734.
- Guzman ML, Li X, Corbett CA, Rossi RM, Bushnell T, Liesveld JL, HÃ©bert J, Young F, Jordan CT. 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). Blood. 2007 Dec 15;110(13):4436-44. Epub 2007 Sep 4. PubMed PMID: 17785584; PubMed Central PMCID: PMC2234782.
- Fink MP. What do insulin, estrogen, valproic acid, and TDZD-8 have in common? Crit Care Med. 2005 Sep;33(9):2115-7. PubMed PMID: 16148489.
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