TDZD-8 | NP 01139 | GSK-3 Inhibitor | AmBeed-信号通路专用抑制剂

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TDZD-8 99%+

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 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： 99%+ 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Cell,2024. Ambeed. [ A125712 ]; • Cancer Discov., 2024. Ambeed. [ A285925 ]; • JMC, 2024, 67(17): 14974-14985. Ambeed. [ A288696 ]; • JMC, 2024, 67(17): 15061-15079. Ambeed. [ A524399 , A633512 , A144280 , A174613 ]; • EJNMMI Radiopharm. Chem., 2024, 9, 61. Ambeed. [ A1257961 , A622068 ]; 更多 >

GSK-3 亚型比较

产品名称	GSK-3 ↓ ↑	GSK-3α ↓ ↑	GSK-3β ↓ ↑	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

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

TDZD-8 99%+

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TDZD-8 99%+

TDZD-8 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

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TDZD-8 生物活性

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TDZD-8 技术信息

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