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TDZD-8 {[allProObj[0].p_purity_real_show]}

货号:A251413 同义名: 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.

TDZD-8 化学结构 CAS号:327036-89-5
TDZD-8 化学结构
CAS号:327036-89-5
TDZD-8 3D分子结构
CAS号:327036-89-5
TDZD-8 化学结构 CAS号:327036-89-5
TDZD-8 3D分子结构 CAS号:327036-89-5
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TDZD-8 纯度/质量文件 产品仅供科研

货号:A251413 标准纯度: {[allProObj[0].p_purity_real_show]}
批次查询: 批次纯度:

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产品名称 GSK-3 GSK-3α GSK-3β 其他靶点 纯度
AZD2858 +

GSK-3, IC50: 68 nM

98+%
Bikinin 99%+
GSK 3 Inhibitor IX ++++

GSK-3, IC50: 5 nM

99%+
AZD1080 +++

GSK-3α, IC50: 6.9 nM

++

GSK-3β, IC50: 31 nM

99%+
BIO-acetoxime +++

GSK-3α, IC50: 10 nM

+++

GSK-3β, IC50: 10 nM

95%
SB-216763 ++

GSK-3α, IC50: 34.3 nM

++

GSK-3β, IC50: ~34.3 nM

98%
SB 415286 +

GSK-3α, IC50: 78 nM

+

GSK-3β, IC50: ~78 nM

99%+
CHIR-98014 ++++

GSK-3α, IC50: 0.65 nM

++++

GSK-3β, IC50: 0.58 nM

98%
LY2090314 ++++

GSK-3α, IC50: 1.5 nM

++++

GSK-3β, IC50: 0.9 nM

99%+
CHIR 99021 +++

GSK-3α, IC50: 10 nM

++++

GSK-3β, IC50: 6.7 nM

99%+
TDZD-8 +

GSK-3β, IC50: 2 μM

99%+
Indirubin +

GSK-3β, IC50: 0.6 μM

98%
IM-12 ++

GSK-3β, IC50: 53 nM

98%
TWS119 ++

GSK-3β, IC50: 30 nM

98%
1-Azakenpaullone +++

GSK-3β, IC50: 18 nM

99%+
AR-A014418 ++

GSK-3β, Ki: 38 nM

99%+
Tideglusib +

GSK-3β, IC50: 60 nM

98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

TDZD-8 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.

TDZD-8 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.

TDZD-8 实验方案

计算器
存储液制备 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

TDZD-8 技术信息

CAS号327036-89-5
分子式C10H10N2O2S
分子量 222.264
别名 NP 01139;GSK-3β Inhibitor I;TDZD 8. GSK3 Inhibitor I
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

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

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
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