CAS:327036-89-5TDZD-8

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Synonyms: NP 01139;GSK-3β Inhibitor I

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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18817579266

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18817579266

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实验数据

技术信息

CAS号

327036-89-5

储存条件

分子式

C10H10N2O2S

运输

蓝冰

分子量

222.26

别名

NP 01139;GSK-3β Inhibitor I

溶解度

动物实验配方

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.