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CAS No.: 327036-89-5

TDZD-8 Catalog No. CSN19500

Synonyms: GSK-3β Inhibitor I;NP 01139

TDZD-8, the derivative of thiadiazolidinone, is a selective inhibitor of GSK-3. It inhibits GSK-3β with IC50 of 2 μM.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 GSK-3β

IC50:2μM
描述TDZD-8 is the first non-ATP competitive inhibitor of GSK-3β with IC50 value of 2μM. Pretreatment with TDZD-8 at 10μM for 1h showed neuroprotection against 6-OHDA-induced damage, shown by reduced cell death and apoptosis, in both SH-SY5Y cells and cultured CGNs. Intrahippocampal delivery of TDZD-8 blocked dephosphorylation and activation of GSK3β in db/db mice. This inhibition of GSK3β prevented accumulation of pS202Tau and hyperphosphorylation of pS396/404Tau in db/db mice. It also reduced somatodendritic tau phosphorylation in db/db mice. The normalization of spatial recognition memory in db/db mice and block of deficits in novel object study could also be observed. Recent study found that TDZD-8 showed inhibition effect on 2019-nCoV.
作用机制TDZD-8 is a non-ATP competitive GSK-3β inhibitor.
参考文献

[1] Guzman ML, Li X, et al. 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.
[2] Martinez A, Alonso M, et al. First non-ATP competitive glycogen synthase kinase 3 beta (GSK-3beta) inhibitors: thiadiazolidinones (TDZD) as potential drugs for the treatment of Alzheimer's disease. J Med Chem. 2002 Mar 14;45(6):1292-9.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 4.4992 mL
- 22.4958 mL
- 44.9916 mL
- 5 mM
- 0.8998 mL
- 4.4992 mL
- 8.9983 mL
- 10 mM
- 0.4499 mL
- 2.2496 mL
- 4.4992 mL

技术信息

CAS号

327036-89-5

储存条件

粉末: Keep in dark place,Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C10H10N2O2S

运输

蓝冰

分子量

222.26

别名

GSK-3β Inhibitor I;NP 01139

溶解度

DMSO	44.5 mg/mL (200.2 mM)
Water	Insoluble
Ethanol	44.0 mg/mL (198.0 mM)

动物实验配方

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