1. PI3K/Akt/mTOR Stem Cell/Wnt
  2. GSK-3
  3. GSK-3β inhibitor 17

GSK-3β inhibitor 17 (compound 5 n) 是一种有效的 GSK-3β 抑制剂。GSK-3β inhibitor 17 可降低顺铂 (HY-17394) 诱导的 p-p65、KIM-1 蛋白和 mRNA 表达。GSK-3β inhibitor 17 可降低顺铂诱导的 TNF-α、IL-1β、IL-6 和 MCP-1 mRNA 表达。GSK-3β inhibitor 17 具有抗炎作用,具有研究急性肾损伤的潜力。

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GSK-3β inhibitor 17 Chemical Structure

GSK-3β inhibitor 17 Chemical Structure

CAS No. : 2521624-67-7

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生物活性

GSK-3β inhibitor 17 (compound 5 n) is a potent GSK-3β inhibitor. GSK-3β inhibitor 17 decreases cisplatin (HY-17394) induced p-p65, KIM-1 protein and mRNA expression. GSK-3β inhibitor 17 decreases cisplatin induced TNF-α, IL-1β, IL-6 and MCP-1 mRNA expression. GSK-3β inhibitor 17 shows anti-inflammation effect and has the potential for the research of acute kidney injury[1].

IC50 & Target[1]

GSK-3β

 

体外研究
(In Vitro)

GSK-3β inhibitor 17 (compound 5 n) (16, 32, 64 µM) 以剂量依赖性方式降低顺铂 (HY-17394) 诱导的 p-p65、KIM-1 蛋白表达[1]
GSK-3β inhibitor 17 (32 µM) 降低顺铂诱导的 HK-2 细胞急性肾损伤 (AKI) 模型中的 TNF-α、IL-1β、IL-6 和 MCP-1 mRNA 表达水平[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: HK-2 cells
Concentration: 16, 32, 64 µM
Incubation Time:
Result: Decreased the cisplatin (20 µM; 24 h) induced protein expression of p-p65, KIM-1.
体内研究
(In Vivo)

GSK-3β inhibitor 17 (12.5, 25, 50 mg/kg; i.p.) 可降低顺铂 (HY-17394) 诱导的 NF-κB 信号激活和炎症细胞因子释放,从而减轻肾损伤[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 6-8 weeks, 20-22 g, Male C57/BL6 mice (cisplatin 20 mg/kg i.p. for 3 days)[1]
Dosage: 12.5, 25, 50 mg/kg
Administration: I.p.; 24 h before the modeling
Result: Inhibited cisplatin-induced renal glycogen accumulation and tubular necrosis, 5n significantly reduced the protein level of p-P65 in cisplatin treatment, significantly downregulated mRNA levels of TNF-α, IL-1β, IL-6 and MCP-1.
分子量

617.58

Formula

C26H18F3N5O6S2

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献

GSK-3β inhibitor 17 相关分类

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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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HY-163748
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