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TDZD-8

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Chemical Structure| 327036-89-5 同义名 : NP 01139;GSK-3β Inhibitor I;TDZD 8. GSK3 Inhibitor I
CAS号 : 327036-89-5
货号 : A251413
分子式 : C10H10N2O2S
纯度 : 99%+
分子量 : 222.264
MDL号 : MFCD04973552
存储条件：

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

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(472.41 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • GSK-3β

    GSK-3β, IC50:2 μM
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.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.50mL

0.90mL

0.45mL

22.50mL

4.50mL

2.25mL

44.99mL

9.00mL

4.50mL
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.