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- 2025年07月09日
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- 详细信息
- 文献和实验
- 技术资料
- 保存条件：
Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 6 months; -20°C, 1 month.
- 英文名：
GSK-3β Inhibitor I; NP 01139
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
327036-89-5
- 规格：
10 mM * 1 mL/1 mg/5 mg/10 mg/25 mg/50 mg/100 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥605.0 |
|---|---|---|---|
| 规格： | 1 mg | 产品价格： | ￥190.0 |
| 规格： | 5 mg | 产品价格： | ￥550.0 |
| 规格： | 10 mg | 产品价格： | ￥800.0 |
| 规格： | 25 mg | 产品价格： | ￥1500.0 |
| 规格： | 50 mg | 产品价格： | ￥2500.0 |
| 规格： | 100 mg | 产品价格： | ￥3500.0 |
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TDZD-8
CAS No. : 327036-89-5
MCE 国际站：TDZD-8
产品活性：TDZD-8 是 GSK-3β 的抑制剂，IC50 为 2 μM；TDZD-8 对 Cdk-1/cyclin?B，CK-II，PKA 和 PKC 的作用较弱，IC50 值均 >100 μM。
研究领域：PI3K/Akt/mTOR | Stem Cell/Wnt
作用靶点：GSK-3
In Vitro: TDZD8 results in a significant decline of cellular ATP levels in PC-3 cells. TDZD8 (10 μM) treatment also triggers a drastic autophagy response and AMPK activation in PC-3 cells. Furthermore, TDZD8 (10 μM) reduces mTOR phosphorylation levels at the S2448 site. In addition, TDZD8 (10 μM) induces LKB1 nuclear-cytoplasm translocation.
In Vivo: TDZD-8 (TDZD8, 1 or 2 mg/kg, i.p.) both reduces the induction of p-DARPP32 following chronic L-dopa treatment in parkinsonian animals. TDZD8 treatment of 21 days induces a significant reduction in PKA expression in rats with established dyskinesia. Moreover, TDZD8 reduces FosB mRNA level in the striatum and lowers the expression of PPEB mRNA to similar levels as in 6-OHDA-lesioned rats without treated with L-dopa. The decrease in dyskinesia induced by TDZD8 is overcome by dopamine rceptor-1 agonist.
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文献和实验kinase assays toward cdk2, cdk5, and25 other kinases (23) . Currently thiadiazolidinone (TDZD) isthe only ATP-noncompetitive inhibitor of GSK-3 (24) . While theexact mechanism by which TDZD inhibits GSK-3 kinase activityis unclear, it has been suggested
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